A sequence-related subfamily of ATP-BINDING CASSETTE TRANSPORTERS that actively transport organic substrates. Although considered organic anion transporters, a subset of proteins in this family have also been shown to convey drug resistance to neutral organic drugs. Their cellular function may have clinical significance for CHEMOTHERAPY in that they transport a variety of ANTINEOPLASTIC AGENTS. Overexpression of proteins in this class by NEOPLASMS is considered a possible mechanism in the development of multidrug resistance (DRUG RESISTANCE, MULTIPLE). Although similar in function to P-GLYCOPROTEINS, the proteins in this class share little sequence homology to the p-glycoprotein family of proteins.
The state of weariness following a period of exertion, mental or physical, characterized by a decreased capacity for work and reduced efficiency to respond to stimuli.
Simultaneous resistance to several structurally and functionally distinct drugs.
A 170-kDa transmembrane glycoprotein from the superfamily of ATP-BINDING CASSETTE TRANSPORTERS. It serves as an ATP-dependent efflux pump for a variety of chemicals, including many ANTINEOPLASTIC AGENTS. Overexpression of this glycoprotein is associated with multidrug resistance (see DRUG RESISTANCE, MULTIPLE).
A family of MEMBRANE TRANSPORT PROTEINS that require ATP hydrolysis for the transport of substrates across membranes. The protein family derives its name from the ATP-binding domain found on the protein.
A subfamily of transmembrane proteins from the superfamily of ATP-BINDING CASSETTE TRANSPORTERS that are closely related in sequence to P-GLYCOPROTEIN. When overexpressed, they function as ATP-dependent efflux pumps able to extrude lipophilic drugs, especially ANTINEOPLASTIC AGENTS, from cells causing multidrug resistance (DRUG RESISTANCE, MULTIPLE). Although P-Glycoproteins share functional similarities to MULTIDRUG RESISTANCE-ASSOCIATED PROTEINS they are two distinct subclasses of ATP-BINDING CASSETTE TRANSPORTERS, and have little sequence homology.
Databases containing information about PROTEINS such as AMINO ACID SEQUENCE; PROTEIN CONFORMATION; and other properties.
A dipolar ionic buffer.
Amino acids that are not synthesized by the human body in amounts sufficient to carry out physiological functions. They are obtained from dietary foodstuffs.
Tumors or cancer of the COLON.
The bestowing of tangible or intangible benefits, voluntarily and usually without expectation of anything in return. However, gift giving may be motivated by feelings of ALTRUISM or gratitude, by a sense of obligation, or by the hope of receiving something in return.
The reciprocal interaction of physicians and nurses.
The ability of bacteria to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).
Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).
Botanically, a type of single-seeded fruit in which the pericarp enclosing the seed is a hard woody shell. In common usage the term is used loosely for any hard, oil-rich kernel. Of those commonly eaten, only hazel, filbert, and chestnut are strictly nuts. Walnuts, pecans, almonds, and coconuts are really drupes. Brazil nuts, pistachios, macadamias, and cashews are really seeds with a hard shell derived from the testa rather than the pericarp.
Diminished or failed response of an organism, disease or tissue to the intended effectiveness of a chemical or drug. It should be differentiated from DRUG TOLERANCE which is the progressive diminution of the susceptibility of a human or animal to the effects of a drug, as a result of continued administration.
Proto-oncogene proteins that negatively regulate RECEPTOR PROTEIN-TYROSINE KINASE signaling. It is a UBIQUITIN-PROTEIN LIGASE and the cellular homologue of ONCOGENE PROTEIN V-CBL.
A plant genus of the family ZINGIBERACEAE that contains CURCUMIN and curcuminoids.
Sorbitan mono-9-octadecanoate poly(oxy-1,2-ethanediyl) derivatives; complex mixtures of polyoxyethylene ethers used as emulsifiers or dispersing agents in pharmaceuticals.
A highly conserved 76-amino acid peptide universally found in eukaryotic cells that functions as a marker for intracellular PROTEIN TRANSPORT and degradation. Ubiquitin becomes activated through a series of complicated steps and forms an isopeptide bond to lysine residues of specific proteins within the cell. These "ubiquitinated" proteins can be recognized and degraded by proteosomes or be transported to specific compartments within the cell.
Chinese herbal or plant extracts which are used as drugs to treat diseases or promote general well-being. The concept does not include synthesized compounds manufactured in China.
Unctuous combustible substances that are liquid or easily liquefiable on warming, and are soluble in ether but insoluble in water. Such substances, depending on their origin, are classified as animal, mineral, or vegetable oils. Depending on their behavior on heating, they are volatile or fixed. (Dorland, 28th ed)
A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.
The third type of glial cell, along with astrocytes and oligodendrocytes (which together form the macroglia). Microglia vary in appearance depending on developmental stage, functional state, and anatomical location; subtype terms include ramified, perivascular, ameboid, resting, and activated. Microglia clearly are capable of phagocytosis and play an important role in a wide spectrum of neuropathologies. They have also been suggested to act in several other roles including in secretion (e.g., of cytokines and neural growth factors), in immunological processing (e.g., antigen presentation), and in central nervous system development and remodeling.
A synthetic amino acid that depletes glutathione by irreversibly inhibiting gamma-glutamylcysteine synthetase. Inhibition of this enzyme is a critical step in glutathione biosynthesis. It has been shown to inhibit the proliferative response in human T-lymphocytes and inhibit macrophage activation. (J Biol Chem 1995;270(33):1945-7)
A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666)
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.
A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)

Overexpression of the multidrug resistance-associated protein (MRP1) in human heavy metal-selected tumor cells. (1/1752)

Cellular and molecular mechanisms involved in the resistance to cytotoxic heavy metals remain largely to be characterized in mammalian cells. To this end, we have analyzed a metal-resistant variant of the human lung cancer GLC4 cell line that we have selected by a step-wise procedure in potassium antimony tartrate. Antimony-selected cells, termed GLC4/Sb30 cells, poorly accumulated antimony through an enhanced cellular efflux of metal, thus suggesting up-regulation of a membrane export system in these cells. Indeed, GLC4/Sb30 cells were found to display a functional overexpression of the multidrug resistance-associated protein MRP1, a drug export pump, as demonstrated by Western blotting, reverse transcriptase-polymerase chain reaction and calcein accumulation assays. Moreover, MK571, a potent inhibitor of MRP1 activity, was found to markedly down-modulate resistance of GLC4/Sb30 cells to antimony and to decrease cellular export of the metal. Taken together, our data support the conclusion that overexpression of functional MRP1 likely represents one major mechanism by which human cells can escape the cytotoxic effects of heavy metals.  (+info)

Characterization of a leukotriene C4 export mechanism in human platelets: possible involvement of multidrug resistance-associated protein 1. (2/1752)

Platelets express leukotriene (LT) C4 synthase and can thus participate in the formation of bioactive LTC4. To further elucidate the relevance of this capability, we have now determined the capacity of human platelets to export LTC4. Endogenously formed LTC4 was efficiently released from human platelets after incubation with LTA4 at 37 degrees C, whereas only 15% of produced LTC4 was exported when the cells were incubated at 0 degrees C. The activation energy of the process was calculated to 49.9 +/- 7.7 kJ/mol, indicating carrier-mediated LTC4 export. This was also supported by the finding that the transport was saturable, reaching a maximal export rate of 470 +/- 147 pmol LTC4/min x 10(9) platelets. Furthermore, markedly suppressed LTC4 transport was induced by a combination of the metabolic inhibitors antimycin A and 2-deoxyglucose, suggesting energy-dependent export. The presence in platelets of multidrug resistance-associated protein 1 (MRP1), a protein described to be an energy-dependent LTC4 transporter in various cell types, was demonstrated at the mRNA and protein level. Additional support for a role of MRP1 in platelet LTC4 export was obtained by the findings that the process was inhibited by probenecid and the 5-lipoxygenase-activating protein (FLAP) inhibitor, MK-886. The present findings further support the physiological relevance of platelet LTC4 production.  (+info)

MSH3 deficiency is not sufficient for a mutator phenotype in Chinese hamster ovary cells. (3/1752)

In the yeast Saccharomyces cerevisiae, the mutS homolog protein products MSH3 and MSH6, each in cooperation with MSH2, play well-defined and specific roles in the repair of DNA mismatches and nucleotide loops. The discrete functions of the human homologs hMSH3 and hMSH6 are less clear and current evidence suggests that the substrate specificity of these proteins may be less strict. To determine the role of MSH3 in mammalian mismatch repair, we employed MSH3-deficient Chinese hamster ovary (CHO) cell lines. No significant changes in mutation rate were detected in the MSH3-deficient strain and there were no differences in sensitivity to DNA-damaging agents. Further analysis of hprt mutants did not show a MSH3-dependent shift in the mutant spectrum. Interestingly, thorough examination of four dinucleotide microsatellite regions revealed instability at only one locus in one of the MSH3-deficient cell lines. These data support the idea of a high degree of redundancy in the function of the MutS homologs MSH3 and MSH6, at least with respect to the control of microsatellite instability.  (+info)

SecA is required for the insertion of inner membrane proteins targeted by the Escherichia coli signal recognition particle. (4/1752)

Recent work has demonstrated that the signal recognition particle (SRP) is required for the efficient insertion of many proteins into the Escherichia coli inner membrane (IM). Based on an analogy to eukaryotic SRP, it is likely that bacterial SRP binds to inner membrane proteins (IMPs) co-translationally and then targets them to protein transport channels ("translocons"). Here we present evidence that SecA, which has previously been shown to facilitate the export of proteins targeted in a post-translational fashion, is also required for the membrane insertion of proteins targeted by SRP. The introduction of SecA mutations into strains that have modest SRP deficiencies produced a synthetic lethal effect, suggesting that SecA and SRP might function in the same biochemical pathway. Consistent with this explanation, depletion of SecA by inactivating a temperature-sensitive amber suppressor in a secAam strain completely blocked the membrane insertion of AcrB, a protein that is targeted by SRP. In the absence of substantial SecA, pulse-labeled AcrB was retained in the cytoplasm even after a prolonged chase period and was eventually degraded. Although protein export was also severely impaired by SecA depletion, the observation that more than 20% of the OmpA molecules were translocated properly showed that translocons were still active. Taken together, these results imply that SecA plays a much broader role in the transport of proteins across the E. coli IM than has been previously recognized.  (+info)

Studies on time-kill kinetics of different classes of antibiotics against veterinary pathogenic bacteria including Pasteurella, Actinobacillus and Escherichia coli. (5/1752)

A systematic analysis of the bacteriostatic/bactericidal effect of several antibiotics used in veterinary medicine was carried out by time-kill kinetic analysis using P. haemolytica, P. multocida, A. pleuropneumoniae, and E. coli. The antibiotics tested were enrofloxacin, danofloxacin, erythromycin, tilmicosin, penicillin G, ceftiofur and tetracycline. Unexpectedly, the antibiotics well characterized as bacteriostatic agents against human pathogens such as tetracycline and macrolides, showed bactericidal activity against P. haemolytica and A. pleuropneumoniae. In contrast, tetracycline and erythromycin were bacteriostatic and tilmicosin was bactericidal against P. multocida. In addition, P. multocida was killed by fluoroquinolones at a slower rate than the other bacteria. Spectrum analysis revealed that ceftiofur and tilmicosin were good substrates of the universal efflux pump, AcrA/B, but penicillin and tetracycline were not. The fluoroquinolones were modest substrates for AcrA/B.  (+info)

Frequent loss of heterozygosity at the DNA mismatch-repair loci hMLH1 and hMSH3 in sporadic breast cancer. (6/1752)

To study the involvement of DNA mismatch-repair genes in sporadic breast cancer, matched normal and tumoral DNA samples of 22 patients were analysed for genetic instability and loss of heterozygosity (LOH) with 42 microsatellites at or linked to hMLH1 (3p21), hMSH2 (2p16), hMSH3 (5q11-q13), hMSH6 (2p16), hPMS1 (2q32) and hPMS2 (7p22) loci. Chromosomal regions 3p21 and 5q11-q13 were found hemizygously deleted in 46% and 23% of patients respectively. Half of the patients deleted at hMLH1 were also deleted at hMSH3. The shortest regions of overlapping (SRO) deletions were delimited by markers D3S1298 and D3S1266 at 3p21 and by D5S647 and D5S418 at 5q11-q13. Currently, the genes hMLH1 (3p21) and hMSH3 (5q11-q13) are the only known candidates located within these regions. The consequence of these allelic losses is still unclear because none of the breast cancers examined displayed microsatellite instability, a hallmark of mismatch-repair defect during replication error correction. We suggest that hMLH1 and hMSH3 could be involved in breast tumorigenesis through cellular functions other than replication error correction.  (+info)

Expression of multidrug resistance protein-related genes in lung cancer: correlation with drug response. (7/1752)

Recently, cDNAs have been identified that encode four human proteins (MRP2-5) with structural similarity to the multidrug resistance protein (MRP). Preliminary studies have shown that levels of mRNAs encoding MRP2, MRP3, and MRP5, are increased in some drug-selected cell lines, but the correlation of MRP2-5 mRNA levels with drug resistance has not been examined. Using a collection of small cell lung cancer (SCLC) and non-SCLC patient samples and unselected cell lines established from patients at various stages of treatment, we examined the expression of MRP2, MRP3, MRP4, and MRP5, as well as MDR1 and MRP, by PCR. The levels of individual mRNAs were correlated with the sensitivity of these cell lines to doxorubicin (DOX), vincristine, VP-16, and cis-diamminedichloroplatinum(II), as determined by a modified MTT assay. Using both SCLC and non-SCLC cell lines, we confirmed the previously observed correlation of MRP mRNA levels with resistance to DOX (B. G. Campling et al., Clin. Cancer Res., 3:115-122, 1997) and found a strong correlation of MRP3 mRNA levels with resistance of the cell lines to DOX. In addition, the mRNA levels of both MRP and MRP3 correlated with resistance of the cell lines to vincristine, VP-16, and cis-diamminedichloroplatinum(II). These findings are consistent with the suggestion that MRP3, like MRP, may contribute to the drug resistance phenotype of lung cancer cells.  (+info)

Cloning and functional characterization of a new multispecific organic anion transporter, OAT-K2, in rat kidney. (8/1752)

We have isolated a cDNA coding a new organic anion transporter, OAT-K2, expressed specifically in rat kidney. The OAT-K2 cDNA had an open reading frame encoding a 498-amino acid protein (calculated molecular mass of 55 kDa) that shows 91% identity with the rat kidney-specific organic anion transporter, OAT-K1. Reverse transcription-coupled polymerase chain reaction analyses revealed that the OAT-K2 mRNA was expressed predominantly in the proximal convoluted tubules, proximal straight tubules, and cortical collecting ducts. When expressed in Xenopus oocytes, OAT-K2 stimulated the uptake of hydrophobic organic anions, such as taurocholate, methotrexate, folate, and prostaglandin E2, although its homolog OAT-K1 transported methotrexate and folate, but not taurocholate and prostaglandin E2. In MDCK cells stably transfected with the OAT-K1 and OAT-K2 cDNAs, each transporter was localized functionally to the apical membranes and showed transport activity similar to that in the oocyte. Moreover, the efflux of preloaded taurocholate was also enhanced across the apical membrane in OAT-K2 transfectant. The taurocholate transport by OAT-K2-expressing cells showed saturability (Km = 10.3 microM). Several organic anions, bile acids, cardiac glycosides, and steroids had potent inhibitory effects on the OAT-K2-mediated taurocholate transport in the transfectant. These findings suggest that the OAT-K2 participates in epithelial transport of hydrophobic anionic compounds in the kidney.  (+info)

TY - JOUR. T1 - Genomic structure, gene expression, and promoter analysis of human multidrug resistance-associated protein 7. AU - Kao, Hsin Hsin. AU - Chang, Ming Shi. AU - Cheng, Jan Fang. AU - Huang, Jin Ding. PY - 2003/2/13. Y1 - 2003/2/13. N2 - The multidrug resistance-associated protein (MRP) subfamily transporters associated with anticancer drug efflux are attributed to the multidrug-resistance of cancer cells. The genomic organization of human multidrug resistance-associated protein 7 (MRP7) was identified. The human MRP7 gene, consisting of 22 exons and 21 introns, greatly differs from other members of the human MRP subfamily. A splicing variant of human MRP7, MRP7A, expressed in most human tissues, was also characterized. The 1.93-kb promoter region of MRP7 was isolated and shown to support luciferase activity at a level 4- to 5-fold greater than that of the SV40 promoter. Basal MRP7 gene expression was regulated by 2 regions in the 5′-flanking region at -1,780-1,287 bp, and at -611 ...
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Coumarin (1,2-benzopyrone) is a natural compound that has been used as a fragrance in the food and perfume industry and could have therapeutic usefulness in the treatment of lymphedema and different types of cancer. Several previous pharmacokinetic studies of coumarin have been performed in humans, which revealed extensive first-pass metabolism of the compound. 7-Hydroxycoumarin (7-HC) and its glucuronide (7-HC-G) are the main metabolites formed in humans, and via this route, 80 to 90% of the absorbed coumarin is excreted into urine, mainly as 7-HC-G. Active transport processes play a role in the urinary excretion of 7-HC-G; however, until now, the transporters involved remained to be elucidated. In this study, we investigated whether the efflux transporters multidrug resistance-associated proteins (MRP)1-4, breast cancer resistance protein, or P-glycoprotein play a role in 7-HC and 7-HC-G transport. For this purpose, we measured uptake of the metabolites into membrane vesicles overexpressing ...
Multidrug resistance-associated protein (MRP), a member of the ABC superfamily transporters, functions as an ATP-dependent efflux pump that extrudes cytotoxic drugs from the cells. Although glutathione has been considered to play an important role in the function of MRP, there is no convincing evide …
By screening databases of human expressed sequence tags, we have identified three new homologues of MRP1, the gene encoding the multidrug resistance-associated protein, and cMOAT (or MRP2), the canalicular multispecific organic anion transporter gene. We call these new genes MRP3, MRP4, and MRP5. MRP3, like cMOAT, is mainly expressed in the liver. MRP4 is expressed only at very low levels in a few tissues, and MRP5, like MRP1, is expressed in almost every tissue tested. To assess a possible role of these new MRP homologues in multidrug or cisplatin resistance, a large set of resistant cell lines was examined for the (over)expression of MRP1, cMOAT, MRP3, MRP4, and MRP5. We find that even in cells selected for a low level of resistance, several MRP-related genes can be up-regulated simultaneously. However, MRP4 is not overexpressed in any of the cell lines we analyzed; MRP3 and MRP5 are only overexpressed in a few cell lines, and the RNA levels do not seem to correlate with resistance to either ...
Intrathecal methotrexate (MTX) has been associated with severe neurotoxicity. Because carrier-associated removal of MTX from the cerebrospinal fluid (CSF) into blood remains undefined, we determined the expression and function of MTX transporters in rat choroid plexus (CP). MTX neurotoxicity usually manifests as seizures requiring therapy with antiepileptic drugs (AEDs) such as phenobarbital (PB). Because we have demonstrated that PB reduces activity of MTX influx carrier reduced folate carrier (Rfc1) in liver, we investigated the influence of the AEDs PB, carbamazepine (CBZ), or gabapentin on Rfc1-mediated MTX transport in CP. Reverse transcriptase-polymerase chain reaction and Western blot analysis showed similar expression of the MTX influx carrier Rfc1 and organic anion transporter 3 or efflux transporter multidrug resistance-associated protein 1 (Mrp1) and breast cancer resistance protein (Bcrp) in rat CP tissue and choroidal epithelial Z310 cells. Confocal microscopy revealed subcellular ...
Sulfur mustard and nitrogen mustard (mechlorethamine, HN2) are potent vesicants developed as chemical warfare agents. These electrophilic, bifunctional alkylating agents cause skin injury, including inflammation, edema, and blistering. HN2 covalently modifies macromolecules such as DNA, RNA, and proteins or is scavenged by glutathione, forming adducts that can contribute to toxicity. Multidrug resistance-associated protein 1 (Mrp1/MRP1) is a transmembrane ATPase known to efflux glutathione-conjugated electrophiles. In the present studies, we examined the effects of modulating Mrp1-mediated transport activity on the sensitivity of primary and PAM212 mouse keratinocytes to HN2. Primary keratinocytes, and to a lesser extent, PAM212 cells, express Mrp1 mRNA and protein and possess Mrp1 functional activity, as measured by calcein efflux. Sulforaphane, an activator of Nrf2, increased Mrp1 mRNA, protein, and functional activity in primary keratinocytes and PAM212 cells and decreased their sensitivity ...
The drug binding also produces significant displacement of several segments of the backbone. There is a large movement of the segment between Val107 and Leu113 (including the mutated residue Ala109), apparently because the segment between Gln104 and Gln108 becomes helical as a result of drug binding. Some of the side chain atoms appear to become displaced by nearly 3 Å upon drug binding. In addition, the segment between Gly861 and Gly870, just preceding TM helix 8, shows a slight backbone displacement and side chain movement up to 3 Å.. Similar interactions often involving the same set of residues appear to occur with the binding of R6G and Et in our model (not shown). Surprisingly, no acidic residue that would neutralize the positive charges of these dyes was found within 6 Å of the ligand (except Asp566, which is close to the benzoic acid moiety of R6G but more than 11 Å away from its amine nitrogens), although the partially negative π-electron cloud of the phenyl ring of Phe664 is about ...
There is increasing evidence that polymorphisms of the adenosine 5′ triphosphate membrane transporters ABCB1 (P-glycoprotein, MDR1) may affect expression and function, whereas less information is available about the impact of ABCC2 (multidrug resistance-associated protein (MRP2)) single-nucleotide polymorphisms . Particularly, their role in human kidney for drug elimination and in the etiology of renal cell carcinoma is poorly understood. ABCB1 and ABCC2 mRNA and protein expression levels were determined by real-time polymerase chain reaction or immunohistochemistry in kidney cancer and adjacent unaffected cortex tissue of 82 nephrectomized renal cell cancer (RCC) patients (63 clear-cell RCC (CCRCC), 19 non-CCRCC). The DNA of all patients was genotyped for ABCB1 −2352G|A, −692T|C, 2677G|T/A (Ala893Ser/Thr), and 3435C|T, and ABCC2 −24C|T, 1249G|A (Val417Ile) and 3972C|T. ABCB1 and ABCC2 were less expressed in CCRCC than in normal cortex on mRNA as well as on protein level. Although the overall
Rats that consumed a high-fat and high-sucrose diet (HF diet) developed hepatic steatosis. Treatment of HF diet-fed rats with fluvastatin (8 mg/kg) was lethal, followed by an elevation in levels of plasma aspartate aminotransferase and creatine kinase activities and skeletal muscle toxicity. This study was conducted to determine whether nutritional status affects statin-induced adverse effects in rats. Fluvastatin treatment of rats fed the HF diet led to an increase in systemic exposure, suggesting altered metabolism and elimination. In fact, although hepatic multidrug resistance-associated protein (Mrp) 2 and multidrug resistance (Mdr) 1b protein levels were not significantly changed by fluvastatin treatment for 8 days of rats fed a HF diet, the organic anion-transporting protein (Oatp) 1, Mrp3, CYP1A, CYP2C, UDP-glucuronosyltransferase (UGT) 1A1, and UGT1A5 protein levels were moderately decreased and the Oatp2, CYP3A, and UGT2B1 protein levels were markedly suppressed. No significant ...
Jin Yang, Bao-Ling Qiu, Chen-Yan Zhou, Qi Zhou, Jian-Qin Li, Jian Pan, Wei-Ying Gu, Xiao-Fei Qi, Rui-Hua Chen, Yi-Na Niu, CS Chen, Shao-Yan Hu: Expression and clinical value of multidrug resistance-associated proteins (MRP) 1 to 6 in Chinese pediatric patients with B-precursor acute lymphoblastic leukemia. Int J Clin Exp Pathol 2017;10(2):1708-1718. (Abstract IJCEP0044754, Full text PDF ...
ATP-binding cassette domain 2 of multidrug resistance-associated protein. The ABC subfamily C is also known as MRP (multidrug resistance-associated protein). Some of the MRP members have five additional transmembrane segments in their N-terminus, but the function of these additional membrane-spanning domains is not clear. The MRP was found in the multidrug-resistance lung cancer cell in which p-glycoprotein was not overexpressed. MRP exports glutathione by drug stimulation, as well as, certain substrates in conjugated forms with anions, such as glutathione, glucuronate, and sulfate. ...
Here we have examined the role of CK2α in regulating MRP1 function via phosphorylation of Thr249. CK2 kinase plays a major role in cell death/survival decisions; consequently, CK2α subunit knockout mice die in midembryogenesis, whereas CK2α knockdown in cell culture is associated with decreased cell survival (Di Maira et al., 2007; Seldin et al., 2008), and even modest reduction in its expression has a large impact on cancer cell homeostasis (Wang et al., 2001; Seeber et al., 2005; Duncan and Litchfield, 2008; Trembley et al., 2010). Thus, it was not surprising that 50% reduction in CK2α expression in our cells was reflected by increased doxorubicin sensitivity (Fig. 3, A and C; Table 1), significant changes in cells ability to efflux doxorubicin (Fig. 4), and reduced MRP1 transport ability (Fig. 3, E and F).. Cell survival when exposed to a known MRP1 substrate, doxorubicin, was assessed by MTT assay; IC50 and IC90 values were extrapolated from this plot (Fig. 3, A and B; Table 1). Although ...
InterPro provides functional analysis of proteins by classifying them into families and predicting domains and important sites. We combine protein signatures from a number of member databases into a single searchable resource, capitalising on their individual strengths to produce a powerful integrated database and diagnostic tool.
AcrAB is a constitutively expressed, major multidrug efflux system of Escherichia coli. We have purified the cytoplasmic membrane component, AcrB, to near homogeneity, and reconstituted the protein into proteoliposomes. In the presence of ΔpH (outside acid), the protein catalyzed the extrusion of fluorescent phospholipids, which were then trapped by protein-free acceptor vesicles. Known substrates of AcrAB, such as bile acids, erythromycin, and cloxacillin, inhibited this activity. Addition of various drugs to AcrB-containing proteoliposomes, in the presence of ΔpH (inside acid) resulted in proton efflux, suggesting that AcrB is a proton antiporter. Interestingly, fluorescent lipid extrusion was accelerated strongly by the periplasmic protein AcrA in the presence of Mg2+, and at pH 5.0 AcrA alone produced a slow mixing of lipids of different vesicles, without causing the mixing of intravesicular material. These results suggest that AcrA brings two membranes together, and under certain ...
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Introduction Multidrug resistance (MDR) is a major cause of treatment failure and mortality in cancer patients. Breast cancer is the most prevalent cancer among women and the second leading cause of death in cancer. The most widely used treatment of breast cancer is chemotherapy, while the success of chemotherapy in breast cancer patients is also seriously limited by the development of MDR [1]. One well-known mechanism of MDR is the over-expression of ATP-binding cassette transporters such as multidrug resistance gene 1 (MDR1), multidrug resistance-associated protein 1 (MRP1), Sunitinib lung resistance protein (LRP). and the breast cancer resistance protein (BCRP) [2-7]. P-glycoprotein (P-gp), which is encoded by the MDR1, is the most extensively studied drug transporter. It is an integral membrane glycoprotein with a molecular mass of 170 kDa and has been postulated to function as a pump that removes hydrophobic anticancer agents from drug-resistant cells, thus promoting MDR [8]. The novel gene ...
Abstract:. Multidrug resistance-associated protein 2 (Mrp2, ABCC2) and P-glycoprotein (P-gp, ABCB1) constitute essential components of the intestinal biochemical barrier that prevent incorporation of food contaminants, drugs or toxic metabolites into the blood stream. Endotoxemia induced in rats by administration of bacterial lipopolysaccharide (LPS) results in elevated intestinal permeability and toxicity of xenobiotics in part associated with down-regulation of expression and activity of Mrp2 and P-gp. We evaluated the protective effect of glucagon-like peptide 2 (GLP-2), a peptide hormone with enterotrophic properties, on Mrp2 and P-gp alterations induced by single i.p. injection of LPS (5 mg/kg b.wt.) to rats. Two different protocols of GLP-2 administration, namely prevention and reversion, were examined. The prevention protocol consisted of 7s.c. injections of GLP-2 (125 μg/kg b.wt.) administered every 12 h, starting 60 h before LPS administration. The reversion protocol consisted of 2 ...
Rat and mous. e Mrp3 share 88% and 89% similarity with human MRP3 at the protein level, respectively. Mrp3 is localized at the basolateral site of renal tubule cells, enterocytes, cholangiocytes and hepatocytes [1, 2]. Although basal expression of rat Mrp3 is low in the liver, it is induced in cholestatic conditions [3], Mrp2 deficiency [4, 5], and by certain drugs and microsomal enzyme inducers [6-10]. It is interesting to note, however, that levels of Mrp2 and Mrp3 are not always inversely correlated, as physiological Mrp2 deficiency in pregnant rats or downregulation of Mrp2 in obese Zucker rats do not cause upregulation of Mrp3 [11, 12]. Unlike in rat liver, Mrp3 has a constitutively high expression in mouse hepatocytes [13] which can be further induced with chemicals [14] but not by Mrp2 deficiency [15]. Within the kidney, MRP3 can be found in different cell types in humans versus rats. While rat Mrp3 is expressed in both the proximal and distal tubules [2], human MRP3 protein was ...
Josephy, 66 conjugative metabolism, 69 cytochrome P450 superfamily, 76 sharpness of, 64 nucleophilic trapping reactions, 73 oxidative metabolism, 69 reductive metabolism, 66 sulfonation, 71 Metabolomics, definition & basic technologies, 121 Metals, contamination of disgrace during tobacco production, 298 Methanol, aggregate of distribution, 65 Microcystin-LR, 175 MicroRNAs, toxicity markers in blood, 161 Mitochondria role in apoptosis, 113 job in AZT hepatotoxicity, 167 Mitochondrial permeability transition (MPT), 113 Mouse lymphoma assay, 244 Multidrug resistance-associated proteins, 136 Munich Beer Heart. Allowing for regarding mercilessly feigned children, heart transplantation is the at best supportable long-term treatment way out (Kantor et al. Early veno-venous haemodiafiltration for sepsisrelated multiple bureau nonstarter buy tadora 20 mg with amex impotence under 30. Deep planner stimulation (DBS) by Medtronic is approved during the FDA to fire electrical stimulation to structures in ...
Like human MRP2, the rat ortholog also mediates the transport of glutathione, glucuronide and glutathione conjugates, sulfated bile salts and unconjugated organic anions [11, 12]. However, differences in the transport rate between human and rat Mrp2 were observed [13-18]. Such differences can lead to altered pharmacokinetic or toxicological profile of drugs. It is also worth noting that species differences occur not only between human and rat, but among preclinical species as well [19, 20], most likely because of the lower expression level of the protein in dog, rabbit and monkey liver compared to human, rat and mouse [20]. Therefore, the prediction of drug safety from animal studies might not be appropriate without the consideration of differences in function and abundance of the protein across the species.. References. 1. Buchler, M., et al., cDNA cloning of the hepatocyte canalicular isoform of the multidrug resistance protein, cMrp, reveals a novel conjugate export pump deficient in ...
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Sarrazin C, Dvory-Sobol H, Svarovskaia ES, Doehle BP, Pang PS, Chuang SM, et al. Prevalence of Resistance-Associated Substitutions in HCV NS5A, NS5B, or NS3 and Outcomes of Treatment With Ledipasvir and Sofosbuvir. Gastroenterology. 2016 June 11th ed. 2016;151(3):501-512.E1. ...
References for Abcams Recombinant Human MRP2 protein (ab112272). Please let us know if you have used this product in your publication
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MRP4兔多克隆抗体(ab32550)可与大鼠, 人样本反应并经WB实验严格验证,被2篇文献引用。中国75%以上现货,所有产品均提供质保服务,可通过电话、电邮或微信获得本地专属技术支持。
TY - JOUR. T1 - Mutations of the Walker B motif in the first nucleotide binding domain of multidrug resistance protein MRP1 prevent conformational maturation. AU - Cui, L.. AU - Hou, Y. X.. AU - Riordan, J. R.. AU - Chang, X. B.. PY - 2001/8/1. Y1 - 2001/8/1. N2 - ATP-binding cassette (ABC) transporters couple the binding and hydrolysis of ATP to the translocation of solutes across biological membranes. The so-called Walker motifs in each of the nucleotide binding domains (NBDs) of these proteins contribute directly to the binding and the catalytic site for the MgATP substrate. Hence mutagenesis of residues in these motifs may interfere with function. This is the case with the MRP1 multidrug transporter. However, interpretation of the effect of mutation in the Walker B motif of NBD1 (D792L/D793L) was confused by the fact that it prevented biosynthetic maturation of the protein. We have determined now that this latter effect is entirely due to the D792L substitution. This variant is unable to ...
The human Dubin-Johnson syndrome and its animal model, the TR− rat, are characterized by a chronic conjugated hyperbilirubinemia. TR− rats are defective in the canalicular multispecific organic anion transporter (cMOAT), which mediates hepatobiliary excretion of numerous organic anions. The complementary DNA for rat cmoat, a homolog of the human multidrug resistance gene (hMRP1), was isolated and shown to be expressed in the canalicular membrane of hepatocytes. In the TR− rat, a single-nucleotide deletion in this gene resulted in a reduced messenger RNA level and absence of the protein. It is likely that this mutation accounts for the TR− phenotype.. ...
TY - JOUR. T1 - Loss of ATP-dependent transport activity in pseudoxanthoma elasticum-associated mutants of human ABCC6 (MRP6). AU - Iliás, Attila. AU - Urbán, Zsolt. AU - Seidl, Thomas L.. AU - Saux, Olivier Le. AU - Sinkó, Emese. AU - Boyd, Charles D.. AU - Sarkadi, B.. AU - Váradi, A.. PY - 2002/5/10. Y1 - 2002/5/10. N2 - Mutations in the ABCC6 (MRP6) gene cause pseudoxanthoma elasticum (PXE), a rare heritable disorder resulting in the calcification of elastic fibers. In the present study a cDNA encoding a full-length normal variant of ABCC6 was amplified from a human kidney cDNA library, and the protein was expressed in Sf9 insect cells. In isolated membranes ATP binding as well as ATP-dependent active transport by ABCC6 was demonstrated. We found that glutathione conjugates, including leukotriene C4 and N-ethylmaleimide S-glutathione (NEM-GS), were actively transported by human ABCC6. Organic anions (probenecid, benzbromarone, indomethacin), known to interfere with glutathione conjugate ...
Identification and characterisation of a new multidrug resistance protein at the blood brain barrier [Elektronische Ressource] / vorgelegt von Tanja Eisenblätter : TANJA EISENBLÄTTER IDENTIFICATION AND CHARACTERISATION OF A NEW MULTIDRUG RESISTANCE PROTEIN AT THE BLOOD-BRAIN BARRIER 2002 Biochemie IDENTIFICATION AND CHARACTERISATION OF A NEW MULTIDRUG RESISTANCE PROTEIN AT THE BLOOD-BRAIN BARRIER Inaugural-Dissertation zur Erlangung des Doktorgrades der Naturwissenschaften im Fachbereich Chemie und Pharmazie der
TY - JOUR. T1 - High incidence of c-jun kinase activity in 2/relapsed acute leukemia. T2 - role in mrp-mediated drug resistance?. AU - Cripe, L. D.. AU - Burgess, O. S.. AU - Tanzer, L.. AU - Kneebpne, P.. AU - Williamson, E. A.. AU - Kraft, A. S.. AU - Moore, R. E.. AU - Boswell, H. S.. N1 - Copyright: Copyright 2006 Elsevier B.V., All rights reserved.. PY - 1997. Y1 - 1997. N2 - Multidrug resistance in leukemia has been attributed to expression of the p-glycoprotein, product of the mdrl gene, or to high expression of bcl-2, an anti-apoptotic effector protein. However, expression of these two effectors is highly restricted within certain leukcmic FAB types, and their frequency does not adequately explain many cases of treatment failure. We hypothesized that failure of induction therapy with cytosine arabinoside plus anthracycline may more commonly follow glutathione (GSH)-dependent drug export by the multidrug resistance-related protein (MRP), and that MRP expression, expression of enzymes such ...
The activity of P-glycoprotein (Pgp/MDR1/ABCB1) and multidrug resistance proteins (MRP/ABCC) influence the pharmacokinetics and bioavailability of many drugs. Few suitable cell lines for the study of drug transport exist. Additional non-human cell lines may help clarify species differences and contribute to the current knowledge of drug transport. The aim of the present study was to characterize three rat epithelial cell lines for transporter expression and activity. Transporter expression was assessed in intestinal IEC-6 and renal GERP and NRK-52E cells using RT-PCR and Western blot analysis. Pgp and Mrp transport activity were analyzed by measuring calcein accumulation and glutathione-S-bimane efflux, respectively. The three cell lines showed Pgp expression and Pgp-dependent transport, both decreasing with culture time after reaching confluency. Besides Pgp, cells expressed Mrp1, Mrp3, Mrp4, and Mrp5, while Mrp2 and Mrp6 were absent. In addition, they showed temperature- and Mrp-dependent ...
[18F]Fluciclovine (trans-1-amino-3-[18F]fluorocyclobutanecarboxylic acid; anti-[18F]FACBC), a positron emission tomography tracer used for the diagnosis of recurrent prostate cancer, is transported via amino acid transporters (AATs) with high affinity (Km: 97-230 μM). However, the mechanism underlying urinary excretion is unknown. In this study, we investigated the involvement of AATs and drug transporters in renal [18F]fluciclovine reuptake. [14C]Fluciclovine (trans-1-amino-3-fluoro[1-14C]cyclobutanecarboxylic acid) was used because of its long half-life. The involvement of AATs in [14C]fluciclovine transport was measured by apical-to-basal transport using an LLC-PK1 monolayer as model for renal proximal tubules. The contribution of drug transporters herein was assessed using vesicles/cells expressing the drug transporters P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), multidrug resistance-associated protein 4 (MRP4), organic anion transporter 1 (OAT1), organic anion transporter 3
Different mechanisms in cancer cells become resistant to one or more chemotherapeutics is known as multidrug resistance(MDR) which hinders chemotherapy efficacy. Potential factors for MDR includes enhanced drug detoxification, decreased drug uptake, increased intracellular nucleophiles levels, enhanced repair of drug induced DNA damage, overexpression of drug transporter such as P-glycoprotein(P-gp), multidrug resistance-associated proteins(MRP1, MRP2) and breast cancer resistance protein(BCRP). Currently nanoassemblies such as polymeric/solid lipid/inorganic/metal nanoparticles, quantum dots, dendrimers, liposomes, micelles has emerged as an innovative, effective and promising platforms for treatment of drug resistant cancer cells. Nanocarriers have potential to improve drug therapeutic index, ability for multifunctionality, divert ABC-transporter mediated drug efflux mechanism and selective targeting to tumor cells, cancer stem cells, tumor initiating cells or cancer microenvironment. Selective
Cellular and regional specific changes in multidrug efflux transporter expression during recovery of vasogenic edema in the rat hippocampus and piriform cortex;kpubs;kpubs.org
Glioblastoma multiforme (GBM) is a highly aggressive brain cancer with extremely poor prognostic outcome despite intensive treatment. All chemotherapeutic agents currently used have no greater than 30-40% response rate, many fall into the range of 10-20%, with delivery across the blood brain barrier (BBB) or chemoresistance contributing to the extremely poor outcomes despite treatment. Increased expression of the multidrug resistance protein 1(MRP1) in high grade glioma, and its role in BBB active transport, highlights this member of the ABC transporter family as a target for improving drug responses in GBM. In this study we show that small molecule inhibitors and gene silencing of MRP1 had a significant effect on GBM cell response to temozolomide (150µM), vincristine (100nM) and etoposide (2µM). Pre-treatment with Reversan (inhibitor of MRP1 and P-glycoprotein) led to a significantly improved response to cell death in the presence of all three chemotherapeutics, in both primary and recurrent GBM
3. Bodeman, C.E.; Dzierlenga, A.L.; Tally, C.M.; Mulligan, R.M.; Lake, A.D.; Cherrington, N.J.; McKarns, S.C. Differential Regulation of Hepatic Organic cation Transporter 1. Organic Anion-Transporting Polypeptide 1a4, Bile-Salt Export Pump, and Multidrug Resistance-Associated Protein 2.Transporter Expression in Lymphocyte-Deficient Mice Associates with Interleukin-6 Production. J Pharmacol Exp Ther., 2013, 347, 136-144 ...
Dofequidar, also known as MS-209, is a quinolone-derived sphingomyelin synthase inhibitor that blocks P-glycoprotein and multidrug resistance-associated protein-1, is under development by Schering for the potential treatment of multidrug resistant tumors. Dofequidar was found to sensitizes cancer stem-like side population cells to chemotherapeutic drugs by inhibiting ABCG2/BCRP-mediated drug export.
Multidrug resistance-associated proteins 1 (MRP1) is a medication efflux transporter that is implicated in the pathology of many neurological diseases and it is associated with advancement of multidrug level of resistance. become impaired in individuals with Alzheimers disease JNJ-7706621 21 JNJ-7706621 JNJ-7706621 and latest preclinical studies possess provided compelling proof for a job of the transporter in the clearance of amyloid-β (Aβ) peptides from the mind.22 23 non-invasive imaging with positron emission tomography (Family pet) can allow evaluation of MRP1 function and keeps considerable potential as an instrument to elucidate the part of MPR1 in human being diseases also to evaluate experimental remedies targeted at modulating transporter function. To allow quantification of MRP1 function in the mind with Family pet Okamura and co-workers lately applied a book imaging concept known as the metabolite extrusion technique (MEM) which uses pro-drug/drug strategy.24 The technique was ...
Verbrugge SE, Assaraf YG, Dijkmans BA, Scheffer GL, Al M, den Uyl D, Oerlemans R, Chan ET, Kirk CJ, Peters GJ, van der Heijden JW, de Gruijl TD, Scheper RJ, Jansen G. Inactivating PSMB5 Mutations and P-Glycoprotein (Multidrug Resistance-Associated Protein/ATP-Binding Cassette B1) Mediate Resistance to Proteasome Inhibitors: Ex Vivo Efficacy of (Immuno)Proteasome Inhibitors in Mononuclear Blood Cells from Patients with Rheumatoid Arthritis. J Pharmacol Exp Ther. 2012 Apr;341(1):174-82. Epub 2012 Jan 10. (3/13/12 KBj ...
Verbrugge SE, Assaraf YG, Dijkmans BA, Scheffer GL, Al M, den Uyl D, Oerlemans R, Chan ET, Kirk CJ, Peters GJ, van der Heijden JW, de Gruijl TD, Scheper RJ, Jansen G. Inactivating PSMB5 Mutations and P-Glycoprotein (Multidrug Resistance-Associated Protein/ATP-Binding Cassette B1) Mediate Resistance to Proteasome Inhibitors: Ex Vivo Efficacy of (Immuno)Proteasome Inhibitors in Mononuclear Blood Cells from Patients with Rheumatoid Arthritis. J Pharmacol Exp Ther. 2012 Apr;341(1):174-82. Epub 2012 Jan 10. (3/13/12 KBj ...
The AcrAB system of Escherichia coli is a multidrug efflux system composed of an RND-type transporter AcrB and a periplasmic accessory protein AcrA, and pumps out a wide variety of lipophilic and amphiphilic inhibitors directly into the medium, presumably through the TolC outer membrane channel. Acr …
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Chemotherapy of pancreatic cancer often fails due to the development of intrinsic and acquired resistance during drug treatment. Recent studies have suggested that MRP5 conferred resistance to first-l
Bacteria that develop resistance to drugs can cause great problems in the treatment of infections and diseases. Multi-drug resistance bacteria pump the drugs out of their cells through membrane proteins known as transporters. To reveal the structure of these proteins and understand their mechanism it is necessary to isolate the proteins, grow crystals and collect data at powerful X-ray sources. An early success at Diamond Light Source has been achieved with crystals of the multidrug efflux membrane protein AcrB. A native and a substrate bound data sets were collected on beamline I04 to 3.3Å and 3.8Å resolution respectively. The crystals belonged to spacegroup H32 with cell dimensions of (a=b=145.3Å c=519.0Å). The structure was solved using the published AcrB structure1 for molecular replacement. This will provide the groundwork for obtaining the structure of AcrB with other substrates in the translocation channel to shed more information as to the mode of action of this protein.
ABCC10 is an efflux pump that confers multidrug resistance to cells by extruding a variety of natural and nucleosides analogues using energy from ATP hydrolysis. The objective of this project is to understand the detailed relationship between ATP hydrolysis and drug transport for ABCC10 and how ABCC10s ATPase activity is regulated. For this study, we mutated aromatic residues to polar residues in the Nucleotide Binding Domains (NBDs) of ABCC10 to determine how these residues are involved in the transport of ABCC10 substrates. Prior, structural analyses of several bacterial ABC-transporters indicated that aromatic amino acid residues in NBDs are needed for ATP binding and ATP hydrolysis. In these studies, substitution of these aromatic residues completely abolished ATP-dependent transport. Prior work on ABCC1 has shown that substitutions such as W (tryptophan) to C (cytidine) or Y (tyrosine) to C (cytidine) decreased ABCC1s affinity for ATP, and ATP-dependent LTC4 transport activities. ...
InterPro provides functional analysis of proteins by classifying them into families and predicting domains and important sites. We combine protein signatures from a number of member databases into a single searchable resource, capitalising on their individual strengths to produce a powerful integrated database and diagnostic tool.
The expression and function of many multidrug transporters (including ABCB1 and ABCG2) have been studied in human being cancer cells and in mouse and human being adult stem cells. microRNAs verified their immediate participation in the regulations ABCG2 translation. Our results explain the controversy relating to the reflection of the gene and also offer brand-new ideas into translational control of the reflection of membrane layer transporter mRNAs by microRNAs in hESCs. gene in rodents provides not really produced embryonic fatal phenotypes, but network marketing leads to hypersensitivity to nutritional phototoxins and to protoporphyria (4). These Isomalt manufacture data recommend that Abcg2 is normally not really needed for virility or viability in mouse embryos, but might end up being vital in the mobile destiny dedication, difference, and homeostasis of progenitor cells. Certainly, the multidrug efflux pump ABCG2 provides been suggested as a factor as the trigger of the aspect people which ...
Blog on ABCC3 sirna product: The ABCC3 abcc3 (Catalog #MBS8210639) is a siRNA produced from Synthetic and is intended for research pur...
BioAssay record AID 681389 submitted by ChEMBL: TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing HEK-293 cells.
Abcc5 - Abcc5 (untagged) - Mouse ATP-binding cassette, sub-family C (CFTR/MRP), member 5 (Abcc5), transcript variant 2, (10ug) available for purchase from OriGene - Your Gene Company.
Mouse polyclonal antibody raised against a full-length human MRPS28 protein. MRPS28 (NP_054737, 1 a.a. ~ 187 a.a) full-length human protein. (H00028957-B01) - Products - Abnova
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複合型酸化的リン酸化異常(COXPD)は、ミトコンドリアの酸化的リン酸化システムの欠陥により起こる多様な症状を持つ疾患群である。リボソームタンパクの遺伝子(MRPS16 and MRPS22)の変異は、出生前に重症な小児病を引き起こすことが報告されている。また、COXPD患者のミトコンドリアの翻訳伸長因子の遺伝子(GFM1, TUFM, TSFM およびC12orf65)に変異があることも報告されている ...
MAPK is a Ser/Thr protein kinase that is widely expressed in various cells. Through a cascade reaction, the MAPK pathway transduces signals to the cell nucleus to regulate transcription, and therefore influences cell proliferation, apoptosis and differentiation (12). In the MAPK family, ERK1/2, p38 and JNK subfamilies have been extensively investigated. ERK1/2 and p38 are involved in osteogenesis-associated gene expression and bone formation in vivo (13,14). However, the full underlying mechanism of ERK1/2 and p38 pathways in osteogenic differentiation remains contradictory. Li et al (14) revealed that when the ERK1/2 and p38 signaling pathways were inhibited in dental follicle cells, osteogenic differentiation in early, middle and advanced stages was promoted. However, Xiao et al (15) reported that inhibition of ERK1/2 resulted in restrained osteoblast activity and bone formation. Therefore, ERK1/2 may exert positive or negative effects on osteogenic differentiation, which may result from ...
Role of multidrug resistance-associated protein 2". Biochem. Pharmacol. 69 (3): 531-9. doi:10.1016/j.bcp.2004.10.017. PMID ... "Induction of intestinal multidrug resistance-associated protein 2 (Mrp2) by spironolactone in rats". Eur. J. Pharmacol. 623 (1- ... protein structures, functions, and recent progress in inhibitor development". J. Steroid Biochem. Mol. Biol. 125 (1-2): 66-82. ...
Here she studied membrane proteins involved in multi-drug resistance. She was awarded two National Institutes of Health grants ... She is a crystallographer and interested in structural studies of proteins from neglected tropical disease pathogens. Asojo was ... a pathogenesis-related-1 protein from the nematode parasite, Necator americanus, and a vaccine antigen for human hookworm ... purification and crystallization of proteins. She shares equipment with the Sabin Vaccine Institute. Since 2001 she has ...
Multidrug resistance protein- MDR1). Not to be confused with Multidrug resistance-associated protein (MRP1) ENSG00000103222 ... Multidrug resistance-associated protein 1 (MRP1) is a protein that in humans is encoded by the ABCC1 gene. The protein encoded ... Lautier D, Canitrot Y, Deeley RG, Cole SP (October 1996). "Multidrug resistance mediated by the multidrug resistance protein ( ... Deeley RG, Cole SP (June 1997). "Function, evolution and structure of multidrug resistance protein (MRP)". Seminars in Cancer ...
... multidrug resistance-associated protein 1 (MRP1/ABCC1), and breast cancer resistance protein (BCRP/ABCG2) in cancer cells that ... Other ABC transporters that contribute to multidrug resistance are ABCC1 (MRP1) and ABCG2 (breast cancer resistance protein). ... transport protein which was originally called P-glycoprotein (P-gp), but it is also referred to as multidrug resistance protein ... Cells that overexpress this protein exhibit multi-drug resistance. Subfamily ABCC contains thirteen members and nine of these ...
Lu F, Hou YQ, Song Y, Yuan ZJ (January 2013). "TFPI-2 downregulates multidrug resistance protein in 5-FU-resistant human ... P-glycoprotein 1 (permeability glycoprotein, abbreviated as P-gp or Pgp) also known as multidrug resistance protein 1 (MDR1) or ... Members of the MDR/TAP subfamily are involved in multidrug resistance. P-gp is an ATP-dependent drug efflux pump for xenobiotic ... Ueda K, Clark DP, Chen CJ, Roninson IB, Gottesman MM, Pastan I (January 1987). "The human multidrug resistance (mdr1) gene. ...
Members of the MDR/TAP subfamily are involved in multidrug resistance. The protein encoded by this gene is involved in the ... The membrane-associated protein encoded by this gene is a member of the superfamily of ATP-binding cassette (ABC) transporters ... TAP1+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH) This article incorporates text from ... ABC proteins transport various molecules across extra- and intra-cellular membranes. ABC genes are divided into seven distinct ...
Members of the MDR/TAP subfamily are involved in multidrug resistance. This gene is located 7 kb telomeric to gene family ... TAP2 is a gene in humans that encodes the protein Antigen peptide transporter 2. The membrane-associated protein encoded by ... This protein forms a heterodimer with ABCB2 in order to transport peptides from the cytoplasm to the endoplasmic reticulum. ... TAP2+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH) This article incorporates text from ...
Doyle LA, Ross DD (2003). "Multidrug resistance mediated by the breast cancer resistance protein BCRP (ABCG2)". Oncogene. 22 ( ... Ejendal KF, Hrycyna CA (2003). "Multidrug resistance and cancer: the role of the human ABC transporter ABCG2". Curr. Protein ... Alternatively referred to as the breast cancer resistance protein (BCRP), this protein functions as a xenobiotic transporter ... "Breast cancer resistance protein: molecular target for anticancer drug resistance and pharmacokinetics/pharmacodynamics". ...
... is a substrate of CYP3A4 and multidrug resistance-associated protein 2; drugs that inhibit these enzymes will ... It inhibits the following receptor tyrosine kinases: MET (hepatocyte growth factor receptor protein) and VEGFR, RET, GAS6 ... blood or protein in urine, wounds that don't heal well, and facial swelling. Grapefruit and grapefruit juice should be avoided ... and protein appearing in urine. Very common adverse effects (greater than 10% of people) include decreased appetite; low ...
The ATP-binding cassette 4 gene encodes the Multidrug resistance protein 3. ABCB4 is associated with progressive familial ... 2003). "Multidrug resistance 3 gene mutation 1712delT and estrogen receptor alpha gene polymorphisms in Finnish women with ... 2003). "Multidrug resistance 3 gene mutation 1712delT and estrogen receptor alpha gene polymorphisms in Finnish women with ... Members of the MDR/TAP subfamily are involved in multidrug resistance as well as antigen presentation. This gene encodes a full ...
"Caveolin-1 and cancer multidrug resistance: coordinate regulation of pro-survival proteins?". Leukemia Research. 28 (9): 907-8 ... Caveolin-1 is a protein that in humans is encoded by the CAV1 gene. The scaffolding protein encoded by this gene is the main ... amyloid precursor protein,gap junction protein, alpha 1,nitric oxide synthase 2A, epidermal growth factor receptor, endothelin ... The protein links integrin subunits to the tyrosine kinase FYN, an initiating step in coupling integrins to the Ras-ERK pathway ...
Some members of the MDR/TAP subfamily are involved in multidrug resistance. This particular protein is responsible for the ... This membrane-associated protein is a member of the superfamily of ATP-binding cassette (ABC) transporters. ABC proteins ... ABCB11+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH) ABCB11 human gene location in the ... ATP-binding cassette, sub-family B member 11 also known as ABCB11 is a protein which in humans is encoded by the ABCB11 gene. ...
ABCG2 is a protein that is responsible for multidrug resistance in cancer chemotherapy. Increased expression of ABCG2 is found ... Mo, Wei; Zhang, Jian-Ting (30 March 2011). "Human ABCG2: structure, function, and its role in multidrug resistance". ... Since many proteins are structurally similar, especially within the same protein family, Broad-spectrum inhibitors can't always ... CXCR4 is a protein that acts as a coreceptor for the entry of HIV. It has been developed as a drug target for anti-HIV therapy ...
This protein is a member of the MRP subfamily which is involved in multi-drug resistance. The specific function of this protein ... Zelcer N, Saeki T, Bot I, Kuil A, Borst P (2003). "Transport of bile acids in multidrug-resistance-protein 3-overexpressing ... Nies AT, König J, Pfannschmidt M, Klar E, Hofmann WJ, Keppler D (2002). "Expression of the multidrug resistance proteins MRP2 ... König J, Rost D, Cui Y, Keppler D (1999). "Characterization of the human multidrug resistance protein isoform MRP3 localized to ...
The laboratory has specialized in structures of multidrug resistance transporter proteins in bacteria. In 2001, while a faculty ... Ma, C; Chang, G (2004). "Structure of the multidrug resistance efflux transporter EmrE from Escherichia coli". Proc Natl Acad ... Chang and coauthors published papers on the structures of multidrug resistance transporters known as EmrE, and MsbA. Although ... Chang, G (2003). "Structure of MsbA from Vibrio cholera: a multidrug resistance ABC transporter homolog in a closed ...
König J, Nies AT, Cui Y, Leier I, Keppler D (December 1999). "Conjugate export pumps of the multidrug resistance protein (MRP) ... Homolya L, Váradi A, Sarkadi B (2003). "Multidrug resistance-associated proteins: Export pumps for conjugates with glutathione ... with the anionic groups acting as affinity tags for a variety of membrane transporters of the multidrug resistance protein (MRP ... Drug metabolism also affects multidrug resistance in infectious diseases and in chemotherapy for cancer, and the actions of ...
Sikora, C; Turner, R (2005). "Investigation of Ligand Binding to the Multidrug Resistance Protein EmrE by Isothermal Titration ... Non-covalent bonding is critical in maintaining the 3D structure of large molecules, such as proteins and is involved in many ... The researchers maintained a large excess of the ligand over the protein to allowing the binding reaction to go to completion. ... A recent example of the use of this technique was for studying the binding affinity of the protein membrane surrounding ...
Multidrug resistance-associated protein 7 is a protein that in humans is encoded by the ABCC10 gene. The protein encoded by ... 2004). "Analysis of the drug resistance profile of multidrug resistance protein 7 (ABCC10): resistance to docetaxel". Cancer ... 2007). "Multidrug resistance-associated protein 7 expression is involved in cross-resistance to docetaxel in salivary gland ... 2003). "Characterization of the transport properties of human multidrug resistance protein 7 (MRP7, ABCC10)". Mol. Pharmacol. ...
Multidrug resistance-associated protein 9 is a protein that in humans is encoded by the ABCC12 gene. This gene is a member of ... Haimeur A, Conseil G, Deeley RG, Cole SP (2004). "The MRP-related and BCRP/ABCG2 multidrug resistance proteins: biology, ... This gene is a member of the MRP subfamily which is involved in multi-drug resistance. This gene and another subfamily member ... ABC proteins transport various molecules across extra- and intracellular membranes. ABC genes are divided into seven distinct ...
ATP-binding cassette sub-family C member 4 (ABCC4), also known as the multidrug resistance-associated protein 4 (MRP4) or multi ... 2011). "Multidrug resistance protein 4(MRP4/ABCC4) regulates cAMP cellular levels and controls human leukemia cellproliferation ... Brüggemann M, Trautmann H, Hoelzer D, Kneba M, Gökbuget N, Raff T (December 2009). "Multidrug resistance-associated protein 4 ( ... "The multidrug-resistance protein 4 polymorphism is a new factor accounting for thiopurine sensitivity in Japanese patients with ...
This protein is a member of the MRP subfamily which is involved in multidrug resistance. Mutations in this protein cause ... Multidrug resistance-associated protein 6 (MRP6) also known as ATP-binding cassette sub-family C member 6 (ABCC6) and multi- ... The protein encoded by the ABCC6 gene is a member of the superfamily of ATP-binding cassette (ABC) transporters. ABC proteins ... GeneReviews/NIH/NCBI/UW entry on Pseudoxanthoma Elasticum ABCC6+protein,+human at the US National Library of Medicine Medical ...
Multidrug resistance-associated protein 5 is a protein that in humans is encoded by the ABCC5 gene. The protein encoded by this ... This protein is a member of the MRP subfamily which is involved in multi-drug resistance. This protein functions in the ... Jedlitschky G, Burchell B, Keppler D (Sep 2000). "The multidrug resistance protein 5 functions as an ATP-dependent export pump ... homologues of the multidrug resistance-associated protein gene (MRP1), in human cancer cell lines". Cancer Research. 57 (16): ...
"Canalicular multispecific organic anion transporter/multidrug resistance protein 2 mediates low-affinity transport of reduced ... impaired biliary excretion of bilirubin glucuronide is due to a mutation in the canalicular multiple drug-resistance protein 2 ... These conditions are associated with either defective intracellular protein binding (for the second time) or disturbed ... or defective intracellular protein binding. In similar fashion, the conjugated hyperbilirubinemia emerges in case the ...
Members of the MDR/TAP subfamily are involved in multidrug resistance as well as antigen presentation. The function of this ... The membrane-associated protein encoded by this gene is a member of the superfamily of ATP-binding cassette (ABC) transporters ... ABCB9+protein,+human at the US National Library of Medicine Medical Subject Headings (MeSH) Human ABCB9 genome location and ... ABC proteins transport various molecules across extra- and intra-cellular membranes. ABC genes are divided into seven distinct ...
Members of the MDR/TAP subfamily are involved in multidrug resistance as well as antigen presentation. The function of this ... The membrane-associated protein encoded by this gene is a member of the superfamily of ATP-binding cassette (ABC) transporters ... ABC proteins transport various molecules across extra- and intra-cellular membranes. ABC genes are divided into seven distinct ... This protein may also play a role in the transport of phospholipids into mitochondrial membranes. ATP-binding cassette ...
Members of the MDR/TAP subfamily are involved in multidrug resistance as well as antigen presentation. This gene encodes a half ... The membrane-associated protein encoded by this gene is a member of the superfamily of ATP-binding cassette (ABC) transporters ... ABC proteins transport various molecules across extra- and intra-cellular membranes. ABC genes are divided into seven distinct ... GeneReviews/NIH/NCBI/UW entry on X-Linked Sideroblastic Anemia and Ataxia ABCB7+protein,+human at the US National Library of ...
This protein is a member of the MRP subfamily which is involved in multi-drug resistance. This protein is thought to form ATP- ... The protein encoded by this gene is a member of the superfamily of ATP-binding cassette (ABC) transporters. ABC proteins ... 2005). "Towards a proteome-scale map of the human protein-protein interaction network". Nature. 437 (7062): 1173-8. doi:10.1038 ... Protein structure suggests a role as the drug-binding channel-modulating subunit of the extrapancreatic ATP-sensitive potassium ...
"Human multidrug resistance protein 8 (MRP8/ABCC11), an apical efflux pump for steroid sulfates, is an axonal protein of the CNS ... "Role of glutathione in the multidrug resistance protein 4 (MRP4/ABCC4)-mediated efflux of cAMP and resistance to purine ... ATP-binding cassette transporter sub-family C member 11, also MRP8 (Multidrug Resistance-Related Protein 8) is a membrane ... and leukotriene C4 by human multidrug resistance protein 8 (ABCC11)". Molecular Pharmacology. 67 (2): 545-57. doi:10.1124/mol. ...
A recent study found that this resistance is due to expression of multidrug resistance protein 1 (MDR1). Fluorescently labeled ... "Single-cell pharmacokinetic imaging reveals a therapeutic strategy to overcome drug resistance to the microtubule inhibitor ...
"Relationship between chemotherapy response of small cell lung cancer and P-glycoprotein or multidrug resistance-related protein ... MARCKS-related protein is a protein that in humans is encoded by the MARCKSL1 gene. This gene encodes a member of the ... Umekage T, Kato K (1991). "A mouse brain cDNA encodes a novel protein with the protein kinase C phosphorylation site domain ... "Entrez Gene: MARCKSL1 MARCKS-like 1". Yue L, Lu S, Garces J, Jin T, Li J (August 2000). "Protein kinase C-regulated dynamitin- ...
They found that there is higher level expression of both proteins and a multidrug resistance-associated protein 1 (ABCC1) was ... protein processing. • protein maturation. • myeloid dendritic cell differentiation. • autophagy. • protein glycosylation. • ... Gottesman MM, Fojo T, Bates SE (January 2002). "Multidrug resistance in cancer: role of ATP-dependent transporters". Nat. Rev. ... positive regulation of protein kinase activity. • T cell activation involved in immune response. • cellular protein metabolic ...
... core protein - correlates of immunity/correlates of protection - creatinine - cross-resistance - cryotherapy - cryptococcal ... multi-drug rescue therapy - multiple drug-resistant tuberculosis (MDR-TB) - mutation - myalgia - mycobacterium - mycobacterium ... resistance - retina - retinal detachment - retinitis - retrovirus - REV - reverse transcriptase - ribonucleic acid (RNA) - ... proteins - protocol - protozoa - provirus - pruritus - pseudo-Cushing's syndrome - pseudovirion - PUBMED - pulmonary - purified ...
Arch G., III Mainous (2010.). Management of Antimicrobials in Infectious Diseases: Impact of Antibiotic Resistance. Humana Pr. ... "Recent advances in the medical and surgical treatment of multi-drug resistant tuberculosis". Curr Opin Pulm Med. svezak 12 ( ... "Mycobacterial outer membranes: in search of proteins". Trends in Microbiology. svezak 18 (broj 3): str. 109.-116. PMC 2931330 ... impact of antibiotic resistance. (2. prerađeno izdanje izd.). Totowa, N.J.: Humana. str. str. 74.. ISBN 978-1-60327-238-4. http ...
This bacterium has developed multi-drug antibiotic resistance and uses colonization and secreted factors in virulence (enzymes ... The enterococcal surface protein (Esp) allows the bacteria to aggregate and form biofilms. Additional virulence factors include ... A genome-wide E. faecium sRNA study suggested that some sRNAs are linked to the antibiotic resistance and stress response.[7] ... Enterococcus faecium has been a leading cause of multi-drug resistant enterococcal infections over Enterococcus faecalis in the ...
Resistance to puromycin is conferred by the pac gene encoding a puromycin N-acetyl-transferase (PAC) that was found in a ... Deletion of the gene encoding the multidrug efflux pump Pdr5 sensitizes cells to puromycin.[citation needed] ... As puromycin inhibits protein synthesis in eukaryotic cells, researchers were able to show that injections of this drug will ... Puromycin resistance in yeast can also be conferred through expression of the puromycin N-acetyl-transferase (pac) gene.[8] ...
Dalton, J. Antibiotic Resistance of Tuberculosis. The Dartmouth Undergraduate Journal of Science [online]. 2009-02-22 [cit. ... Lalloo, U., Naidoo, R., Ambaram, A. Recent advances in the medical and surgical treatment of multi-drug-resistant tuberculosis ... delivered as naked DNA or recombinant protein. Journal of Immunology. 2004, roč. 172, čís. 12, s. 7618-28. PMID 15187142.. ... Johnson, R., Streicher, E. M., Louw, G. E., Warren, R. M., van Helden, P. D., Victo, T. C. Drug Resistance in Mycobacterium ...
Antibiotic resistance. In many areas of the world, antibiotic resistance is increasing within cholera bacteria. In Bangladesh, ... The bacteria stop producing the protein flagellin to conserve energy and nutrients by changing the mix of proteins that they ... Rapid diagnostic assay methods are available for the identification of multi-drug resistant cases.[34] New generation ... cholerae bacteria turn off the production of some proteins and turn on the production of other proteins as they respond to the ...
... resistance arises due to mutations in penicillin-binding proteins, production of metallo-β-lactamases, or resistance to ... is a potent inducer of multidrug resistance in bacteria. Pharmacology[edit]. Mechanism of action[edit]. Meropenem is ...
McDevitt, R. Callaghan (2009). Multidrug Resistance in Cancer. Generating Inhibitors of P-Glycoprotein: Where to, Now?. ... can occur which prevent the drugs from binding to the protein, leading to resistance to these types of drugs.[117] Drugs used ... Resistance[edit]. Resistance is a major cause of treatment failure in chemotherapeutic drugs. There are a few possible causes ... Goldman B (Feb 2003). "Multidrug resistance: can new drugs help chemotherapy score against cancer?". Journal of the National ...
Fluoroquinolone antibiotics, such as ciprofloxacin or levofloxacin, may no longer be effective in some cases due to resistance. ... "Antimicrobial Susceptibilities of Multidrug-Resistant Campylobacter jejuni and C. coli Strains: In Vitro Activities of 20 ... "Molecular signatures (unique proteins and conserved indels) that are specific for the epsilon proteobacteria ( ...
Multidrug-Resistant "Tuberculosis". Centers for Disease Control and Prevention. Archived March 9, 2010, at the Wayback Machine ... Resistance to infection (immunity) may be acquired following a disease, by asymptomatic carriage of the pathogen, by harboring ... The ability of the viral protein hemagglutinin to bind red blood cells together into a detectable matrix may also be ... Immune resistance to an infectious disease requires a critical level of either antigen-specific antibodies and/or T cells when ...
New emerging pathogen: Candida auris is an emerging multidrug-resistant (MDR) yeast that can cause invasive infections and is ... antifungal resistance, or antifungal intolerance.[4] ... Proteins. LFT. *Elevated transaminases. *Elevated ALP. * ...
Type by resistance. *Multi-drug-resistant tuberculosis. *Extensively drug-resistant tuberculosis. *Totally drug-resistant ... Purified protein derivative (PPD) tuberculin is a precipitate of non-species-specific molecules obtained from filtrates of ... Seibert, F. B.; Glenn, J. T. (1944). "Tuberculin purified protein derivative: preparation and analyses of a large quantity for ... and the purified protein derivative (PPD) tine test. Common brand names of the test include Aplisol, Aplitest, Tuberculin PPD ...
Arch G., III Mainous (2010). Management of Antimicrobials in Infectious Diseases: Impact of Antibiotic Resistance. Humana Pr. s ... Lalloo UG, Naidoo R, Ambaram A (May 2006). "Recent advances in the medical and surgical treatment of multi-drug resistant ... in search of proteins". Trends in Microbiology 18 (3): 109-16. doi:10.1016/j.tim.2009.12.005. PMID 20060722.. ... Centers for Disease Control and Prevention (CDC) (2006). "Emergence of Mycobacterium tuberculosis with extensive resistance to ...
... or having intermediate resistance to an antibiotic.[5] Specific patterns of drug resistance or multi drug resistance may be ... The use of fluorescent dyes has been explored.[9] These involve labelled proteins targeted at biomarkers, nucleic acid ... This resistance might be because a type of bacteria has intrinsic resistance to some antibiotics,[2] because of resistance ... McAdams D (January 2017). "Resistance diagnosis and the changing epidemiology of antibiotic resistance". Annals of the New York ...
The families can be distinguished from one another on the basis of conserved signature indels found among a variety of proteins ... Species within the Stenotrophomonas genus are multidrug resistant opportunistic pathogens that are responsible for nosocomial ... comparative and functional analysis of Stenotrophomonas maltophilia reveals an organism heavily shielded by drug resistance ... "Evolutionary placement of Xanthomonadales based on conserved protein signature sequences". Mol Phylogenet Evol. 54 (2): 524-34 ...
Characterising multidrug resistance (MDR) in cancer cells. *Chromosome analysis and sorting (library construction, chromosome ... Protein modifications, phospho-proteins. *Scattering of light can be used to measure volume (by forward scatter) and ... Transgenic products in vivo, particularly the green fluorescent protein or related fluorescent proteins ... An electrical charging ring is placed just at the point where the stream breaks into droplets. A charge is placed on the ring ...
Development of multidrug resistance by P. aeruginosa isolates requires several different genetic events that include ... This pathogenesis may in part be due to the proteins secreted by P. aeruginosa. The bacterium possesses a wide range of ... Besides intrinsic resistance, P. aeruginosa easily develops acquired resistance either by mutation in chromosomally encoded ... Antibiotic resistanceEdit. Most Pseudomonas spp. are naturally resistant to penicillin and the majority of related beta-lactam ...
... has been studied as part of a multi-drug chemotherapy regimen for drug-resistant T-cell prolymphocytic leukemia.[42] ... is not explained by gene or protein expression. Instead, cladribine appears to deplete the entire B cell department. However, ... "Epigenetic therapy overcomes treatment resistance in T cell prolymphocytic leukemia". Science Translational Medicine. 7 (293 ...
Echinocandins for the treatment of systemic fungal infection , Canadian Antimicrobial Resistance Alliance (CARA) ... "Aspergillus fumigatus: New Opportunities for Treatment of Multidrug-Resistant Fungal Disease". mBio. 8 (4): e01157-17. doi ... Not to be confused with Antifungal protein.. Antifungal. Drug class. Canesten (clotrimazole) antifungal cream ...
Multidrug resistance[edit]. Adult stem cells express transporters of the ATP-binding cassette family that actively pump a ... and their associated proteins between the daughter cells.[3] ... exported by these transporters conferring multidrug resistance ... Chaudhary PM, Roninson IB (July 1991). "Expression and activity of P-glycoprotein, a multidrug efflux pump, in human ... the molecular distinction between symmetric and asymmetric divisions lies in differential segregation of cell membrane proteins ...
In community-acquired infections, they are recommended only when risk factors for multidrug resistance are present or after ... plasmid-mediated resistance genes produce proteins that can bind to DNA gyrase, protecting it from the action of quinolones. ... Antibiotic misuse and bacterial resistances[edit]. See also: Antibiotic misuse and Antibiotic resistance ... M Jacobs, Worldwide Overview of Antimicrobial Resistance. International Symposium on Antimicrobial Agents and Resistance 2005. ...
This rapid evolution is important in medicine, as it has led to the development of multidrug resistant pathogenic bacteria, ... I. Isolation, morphology, cultural characteristics, and resistance to gamma radiation". Food Technol. 10 (1): 575-577.. ... Streptokinase is an extracellular protein, extracted from certain strains of beta hemolytic streptococcus.. ... proteins and metabolites, is utilised by the bacteria to achieve regulation of gene expression. In bacteria, the principal ...
Debry P, Nash EA, Neklason DW, Metherall JE (January 1997). "Role of multidrug resistance P-glycoproteins in cholesterol ... both genetic mutations in hepatocyte proteins involved in bile secretion together with inhibition of those proteins by high ... Genetic mutations in the hepatocellular transport protein ABCB4 (MDR3), which controls secretion of phosphatidylcholine into ...
Type by resistance. *Multi-drug-resistant tuberculosis. *Extensively drug-resistant tuberculosis. *Totally drug-resistant ... Esmond R. Long and Florence B. Seibert identified the active agent in tuberculin as a protein. Seibert then spent a number of ... This is because the immune system needs to be functional to mount a response to the protein derivative injected under the skin ... Purified protein derivative (PPD) tuberculin is a precipitate of species-nonspecific molecules obtained from filtrates of ...
it has been found to specifically inhibit MRP (multidrug resistance proteins) in murine and human cells[15] ... Indomethacin-mediated reversal of multidrug resistance and drug efflux in human and murine cell lines overexpressing MRP, but ... It does so by reducing renal blood flow and increasing renal vascular resistance, possibly by enhancing the effects of ...
Plasmids often carry multiple antibiotic resistance genes, contributing to the spread of multidrug-resistance (MDR). Antibiotic ... Examples of resistance mechanisms include different Qnr proteins, aminoglycose acetyltransferase aac(6')-Ib-cr that is able to ... Multiple resistance genes are commonly arranged in the resistance cassettes. The antibiotic resistance genes found on the ... Plasmid-mediated resistance is the transfer of antibiotic resistance genes which are carried on plasmids. The plasmids can be ...
... namely the multidrug resistance protein 4 (MRP4, ABCC4), a member of the ATP-binding cassette transporter superfamily. Whether ... Prostaglandins ligate a sub-family of cell surface seven-transmembrane receptors, G-protein-coupled receptors. These receptors ...
We combine protein signatures from a number of member databases into a single searchable resource, capitalising on their ... InterPro provides functional analysis of proteins by classifying them into families and predicting domains and important sites ... This entry represents the multidrug resistance-associated protein 5 (MRP5 or ABCC5). It belongs to the MRP (multidrug ... Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs.. Proc. Natl. ...
This protein has an unusually broad substrate specificity and is capable of transporting not only a wide... ... multidrug resistance protein 1 (P-glycoprotein, ABCB1), ABCB-type protein. MDR3. multidrug resistance protein 3 (ABCB4), ABCB- ... Multidrug resistance markers P-glycoprotein, multidrug resistance protein 1, and lung resistance protein in non-small cell lung ... multidrug resistance related protein-1, and lung resistance-related protein expression. Nucl Med Biol 30:627-632PubMedGoogle ...
... Isabella Massimi,1 Ambra Ciuffetta,2 Flavia ... Isabella Massimi, Ambra Ciuffetta, Flavia Temperilli, et al., "Multidrug Resistance Protein-4 Influences Aspirin Toxicity in ...
... the godfather of the family and well known as the multidrug resistance protein, and five homologs, called MRP2-6. In this ... The human multidrug resistance protein (MRP) family contains at least six members: MRP1, ... review, we summarize what is known about the protein structure, the expression in tissues … ... The multidrug resistance protein family Biochim Biophys Acta. 1999 Dec 6;1461(2):347-57. doi: 10.1016/s0005-2736(99)00167-4. ...
Two proteins have been shown to cause this type of multidrug resistance in human tumour cells, the 170 kDa P-glycoprotein and ... Inherent or acquired resistance to multiple natural product drugs is a major obstacle to the success of chemotherapy. ... Multidrug resistance mediated by the multidrug resistance protein (MRP) gene Biochem Pharmacol. 1996 Oct 11;52(7):967-77. doi: ... Two proteins have been shown to cause this type of multidrug resistance in human tumour cells, the 170 kDa P-glycoprotein and ...
Small multidrug resistance protein (also known as Drug/Metabolite Transporter) is a family of integral membrane proteins that ... "Cloning and characterization of the mvrC gene of Escherichia coli K-12 which confers resistance against methyl viologen ... confer drug resistance to a wide range of toxic compounds by removing them for the cells. The efflux is coupled to an influx of ...
Multidrug resistance-associated protein 6Add BLAST. 1498. Amino acid modifications. Feature key. Position(s). Description ... sp,Q9R1S7,MRP6_MOUSE Multidrug resistance-associated protein 6 OS=Mus musculus OX=10090 GN=Abcc6 PE=1 SV=3 ... Protein-protein interaction databases. STRING: functional protein association networks. More...STRINGi. 10090. ... to allow unambiguous identification of a protein.,p>,a href=/help/protein_names target=_top>More...,/a>,/p>Protein namesi. ...
Protein. Similar proteins. Species. Score. Length. Source. A0A2R8YDC1. Isoform 4 of Multidrug resistance-associated protein 4. ... Protein. Similar proteins. Species. Score. Length. Source. A0A2R8YDC1. Isoform 3 of Multidrug resistance-associated protein 4. ... Multidrug resistance-associated pro.... Multidrug resistance-associated protein 4 (ATP-binding cassette sub-family C member 4 ... Multidrug resistance-associated protein 4Imported. ,p>Information which has been imported from another database using automatic ...
2001). "Impaired protein maturation of the conjugate export pump multidrug resistance protein 2 as a consequence of a deletion ... this protein is a member of the MRP subfamily, which is involved in multi-drug resistance. This protein is expressed in the ... 1999). "The human multidrug resistance protein 2 gene: functional characterization of the 5-flanking region and expression in ... Bakos E, Evers R, Sinkó E, Váradi A, Borst P, Sarkadi B (April 2000). "Interactions of the human multidrug resistance proteins ...
Structural model of ATP-binding proteins associated with cystic fibrosis, multidrug resistance and bacterial transport.. Hyde ... and eukaryotic proteins including the P-glycoprotein associated with multidrug resistance in tumours (MDR), the STE6 gene ... The ATP-binding cassette (ABC) superfamily of transport systems now includes over thirty proteins that share extensive sequence ... This superfamily includes the well characterized periplasmic binding protein-dependent uptake systems of prokaryotes, bacterial ...
Multidrug resistance-associated protein 2 (MRP2/ABCC2) is mainly expressed in the apical phase of barrier membranes. It ... Studies on pyrrolopyrimidines as selective inhibitors of multidrug-resistance-associated protein in multidrug resistance. J Med ... Overexpression of multidrug resistance protein gene in human cancer cell lines selected for drug resistance to ... Drug resistance and ATP-dependent conjugate transport mediated by the apical multidrug resistance protein, MRP2, permanently ...
Overexpression of proteins in this class by NEOPLASMS is considered a possible mechanism in the development of multidrug ... resistance (DRUG RESISTANCE, MULTIPLE). Although similar in function to P-GLYCOPROTEINS, the proteins in this class share ... a subset of proteins in this family have also been shown to convey drug resistance to neutral organic drugs. Their cellular ... Multidrug Resistance-Associated Proteins: A sequence-related subfamily of ATP-BINDING CASSETTE TRANSPORTERS that actively ...
Multidrug resistance-associated protein and mutant p53 protein expression in non-small cell lung cancer. Mod Pathol 1998. 11: ... Multidrug resistance-associated protein (MRP) expression is correlated with expression of aberrant p53 protein in colorectal ... Multidrug resistance mediated by the ATP-binding cassette transporter protein MRP. Bioessays 1998. 20:931-940. View this ... Transcriptional suppression of multidrug resistance-associated protein (MRP) gene expression by wild-type p53. Cancer Res 1998 ...
Antifolate Resistance Mediated by the Multidrug Resistance Proteins MRP1 and MRP2. Jan Hendrik Hooijberg, Henk J. Broxterman, ... Antifolate Resistance Mediated by the Multidrug Resistance Proteins MRP1 and MRP2. Jan Hendrik Hooijberg, Henk J. Broxterman, ... Antifolate Resistance Mediated by the Multidrug Resistance Proteins MRP1 and MRP2. Jan Hendrik Hooijberg, Henk J. Broxterman, ... Cross-resistance to antifolates in multidrug resistant cell lines with P-glycoprotein or multidrug resistance protein ...
Multidrug resistance-associated protein 1 (MRP1) is a member of the ATP-binding cassette membrane transport superfamily and is ... functional consequences of mutating cysteine residues in the amino terminus of human multidrug resistance-associated protein 1. ... responsible for multidrug resistance in cancer cells. Currently, there are nine known human MRPs. Distinct from many other ... residue is critical for the MRP1-mediated drug resistance and leukotriene C(4) transport activity. On the other hand, mutation ...
The human multidrug resistance-associated protein MRP confers resistance to various cytotoxic drugs by lowering the ... Basolateral localization and export activity of the human multidrug resistance-associated protein in polarized pig kidney cells ... therefore be useful lead compounds for the development of clinical reversal agents specific for MRP-mediated drug resistance. ...
... ,, Previous Message , Next Message ,, From:. Vaughan, Mary ,[email protected], ... Good Morning David, Ive done several years of Multi Drug Resistance Protein work. It was a tough nut to crack back a few years ... I am trying to locate a good antibody to Multi Drug Resistance Protein that works well on paraffin processed neuroblastoma ... Expression of the MRP and MDR1 Multidrug Resistance Gene Products in 160 Untreated Human Carcinomas Studied by ...
... behave as apoptogens in multidrug resistance protein 1 (MRP1)-expressing cells. When treated with either verapamil or NMeOHI(2 ... Multidrug Resistance-Associated Proteins / genetics, metabolism*. Transfection. Verapamil / analogs & derivatives, pharmacology ... 0/Multidrug Resistance-Associated Proteins; 0/alpha-(3-((2-(4-hydroxy-3,5-diiodophenyl)ethyl)methylamino)propyl) -3,4-dimethoxy ... 0/multidrug resistance-associated protein 1; 52-53-9/Verapamil; 70-18-8/Glutathione; 72025-60-6/Leukotriene C4 ...
What is multidrug resistance-associated protein 4? Meaning of multidrug resistance-associated protein 4 medical term. What does ... Looking for online definition of multidrug resistance-associated protein 4 in the Medical Dictionary? multidrug resistance- ... Multidrug resistance-associated protein 4 , definition of multidrug resistance-associated protein 4 by Medical dictionary https ... redirected from multidrug resistance-associated protein 4) ABCC4. A gene on chromosome 13q32 that encodes a protein of the MRP ...
Keywords: E3 ubiquitin ligase; β-elemene; multidrug resistance; PI3K/Akt E3 ubiquitin ligase; β-elemene; multidrug resistance; ... The Role of E3 Ubiquitin Ligase Cbl Proteins in β-Elemene Reversing Multi-Drug Resistance of Human Gastric Adenocarcinoma Cells ... "The Role of E3 Ubiquitin Ligase Cbl Proteins in β-Elemene Reversing Multi-Drug Resistance of Human Gastric Adenocarcinoma Cells ... The Role of E3 Ubiquitin Ligase Cbl Proteins in β-Elemene Reversing Multi-Drug Resistance of Human Gastric Adenocarcinoma Cells ...
... multidrug resistance protein; hMRP1, human multidrug resistant protein 1; rMRP1, rat multidrug resistance protein 1; HIV-1, ... cloned the first multidrug resistance gene, the product of which is now commonly referred to as the multidrug resistance ... Borst P, Evers R, Kool M, and Wijnholds J (1999) The multidrug resistance protein family. Biochim Biophys Acta 1461: 347-357. ... Functional Expression of the Multidrug Resistance Protein 1 in Microglia. Shannon Dallas, Xiaoping Zhu, Sylvain Baruchel, ...
Showing Protein Multidrug resistance-associated protein 1 (HMDBP01858). IdentificationBiological propertiesGene properties ... Mutation of a single conserved tryptophan in multidrug resistance protein 1 (MRP1/ABCC1) results in loss of drug resistance and ... Identification of an amino acid residue in multidrug resistance protein 1 critical for conferring resistance to anthracyclines ... Zhang DW, Nunoya K, Vasa M, Gu HM, Theis A, Cole SP, Deeley RG: Transmembrane helix 11 of multidrug resistance protein 1 (MRP1/ ...
Ascites Increases Expression/Function of Multidrug Resistance Proteins in Ovarian Cancer Cells. Autoři. LIHONG M.o. ... Ascites Increases Expression/Function of Multidrug Resistance Proteins in Ovarian Cancer Cells ... One mechanism behind chemo-resistance involves the upregulation of multidrug resistance (MDR) genes (ABC transporters) that ... Multidrug Related Protein (MRP1); Breast Cancer Related Protein (BCRP)]. To demonstrate relevance of our findings to ovarian ...
Multidrug resistance protein 2 (MRP2) belongs to the ATP binding cassette family of transporters. Its substrates include ... Evidence for two interacting ligand binding sites in human multidrug resistance protein 2 (ATP binding cassette C2).. [Noam ...
The presence of MK571 (inhibitor of MRP1 and Multidrug resistance protein 4 (MRP4) led to an enhanced effect of vincristine and ... The presence of MK571 (inhibitor of MRP1 and Multidrug resistance protein 4 (MRP4) led to an enhanced effect of vincristine and ... Increased expression of the multidrug resistance protein 1(MRP1) in high grade glioma, and its role in BBB active transport, ... Increased expression of the multidrug resistance protein 1(MRP1) in high grade glioma, and its role in BBB active transport, ...
Functional Expression of the Multidrug Resistance Protein 1 (MRP1) in Microglia. Shannon Dallas, Xiaoping Zhu, Sylvain Baruchel ... Functional Expression of the Multidrug Resistance Protein 1 (MRP1) in Microglia. Shannon Dallas, Xiaoping Zhu, Sylvain Baruchel ... Functional Expression of the Multidrug Resistance Protein 1 (MRP1) in Microglia. Shannon Dallas, Xiaoping Zhu, Sylvain Baruchel ... Functional Expression of the Multidrug Resistance Protein 1 (MRP1) in Microglia Message Subject (Your Name) has forwarded a ...
... we have examined the tissue distribution of gene and protein expression of the multidrug resistance proteins TrnMRP1 and ... Expression of multidrug resistance proteins is localized principally to the Malpighian tubules in larvae of the cabbage looper ... The multidrug resistance proteins (MRPs) serve a number of important roles in development, physiological homeostasis and ... Labbé, R., Caveney, S., Donly, C. (2011). Expression of multidrug resistance proteins is localized principally to the ...
Pillars Article: MHC Class II Region Encoding Proteins Related to the Multidrug Resistance Family of Transmembrane Transporters ... Pillars Article: MHC Class II Region Encoding Proteins Related to the Multidrug Resistance Family of Transmembrane Transporters ... Pillars Article: MHC Class II Region Encoding Proteins Related to the Multidrug Resistance Family of Transmembrane Transporters ... Pillars Article: MHC Class II Region Encoding Proteins Related to the Multidrug Resistance Family of Transmembrane Transporters ...
... whose expression is associated with multidrug resistance, have been recently located in the brain capillary endothelial cells ( ... and the multidrug resistance-associated proteins (MRP), whose expression is associated with multidrug resistance, have been ... Keywords : Blood-brain barrier P-glycoprotein Multidrug resistance-associated protein Endothelial cell Glial cell Pericyte ... Contribution of glial cells and pericytes to the mRNA profiles of P-glycoprotein and multidrug resistance-associated proteins ...
Multidrug Resistance Proteins and the Human Trabecular Meshwork P. A. Knepper; T. Koga; M. J. Nolan; B. Y. J. T. Yue; J. R. ... Multidrug Resistance Proteins and the Human Trabecular Meshwork You will receive an email whenever this article is corrected, ... P. A. Knepper, T. Koga, M. J. Nolan, B. Y. J. T. Yue, J. R. Samples, A. Sheppard, A. F. Clark; Multidrug Resistance Proteins ... multidrug resistance protein (MDR) p-glycoprotein), expression and function are controlled by hyaluronic acid (HA) and the HA ...
  • Borst P, Evers R, Kool M, Wijnholds J. A family of drug transporters: the multidrug resistance-associated proteins. (springer.com)
  • Although considered organic anion transporters, a subset of proteins in this family have also been shown to convey drug resistance to neutral organic drugs. (curehunter.com)
  • A gene on chromosome 13q32 that encodes a protein of the MRP subfamily of the superfamily of ATP-binding cassette (ABC) transporters, which transport various molecules across extra- and intracellular membranes, many of which are involved in multidrug resistance. (thefreedictionary.com)
  • Brain expression of the multidrug resistance proteins (MRPs), a collection of membrane-associated ATP-dependent efflux transporters, is poorly understood. (aspetjournals.org)
  • One mechanism behind chemo-resistance involves the upregulation of multidrug resistance (MDR) genes (ABC transporters) that effectively transport (efflux) drugs out of the tumor cells. (muni.cz)
  • Multidrug resistance protein 2 (MRP2) belongs to the ATP binding cassette family of transporters. (sigmaaldrich.com)
  • Pillars Article: MHC Class II Region Encoding Proteins Related to the Multidrug Resistance Family of Transmembrane Transporters. (jimmunol.org)
  • Lapatinib can modulate the function of ATP-binding cassette (ABC) transporters (ABCB1 and ABCG2), which are the major mechanism responsible for multidrug resistance (MDR) in cancer. (springer.com)
  • Membrane transporters are proteins that play a crucial role in resistance to chemotherapy. (archbronconeumol.org)
  • fnx1 + encodes a protein with sequence similarity to the proton-driven plasma membrane transporters from the multidrug resistance group of the major facilitator superfamily of proteins. (asm.org)
  • In tumor cells, increased expression of these drug transporters is associated with resistance to multiple chemotherapeutic agents. (eurekaselect.com)
  • A. Haimeur, G. Conseil, R. G. Deeley and S. P.C. Cole, " (Section A: Molecular, Structural, and Cellular Biology of Drug Transporters) The MRP-Related and BCRP / ABCG2 Multidrug Resistance Proteins: Biology, Substrate Specificity and Regulation", Current Drug Metabolism (2004) 5: 21. (eurekaselect.com)
  • In vitro, the MRP/ABCC transporters can collectively confer resistance to natural product anticancer drugs and their conjugated metabolites, platinum compounds, folate antimetabolites, nucleoside and nucleotide analogs, arsenical and antimonial oxyanions, peptide-based agents, and in concert with alterations in phase II conjugating or biosynthetic enzymes, classical alkylating agents, alkylating agents. (eurekaselect.com)
  • Drug targeting of these transporters to overcome MRP/ABCC-mediated multidrug resistance may play a role in cancer chemotherapy. (eurekaselect.com)
  • P. falciparum genome analysis has revealed two genes coding for the multidrug resistance protein (MRP) type of ABC transporters: Pfmrp1, previously associated with decreased parasite drug susceptibility, and the poorly studied Pfmrp2. (ntu.edu.sg)
  • The membrane-associated protein encoded by this gene is a member of the superfamily of ATP-binding cassette (ABC) transporters. (nih.gov)
  • Multidrug resistance-associated protein 4 (MRP4) is a member of the C subfamily of the ABC family of ATP-binding cassette (ABC) transporters. (biomedcentral.com)
  • The protein encoded by this gene is a member of the superfamily of ATP-binding cassette (ABC) transporters. (nih.gov)
  • Multidrug resistance protein 5 (MRP5/ABCC5) is a 161 kDa member of the super family of ATP-binding cassette (ABC) superfamily of transmembrane transporters that is clinically relevant for its ability to confer multidrug resistance by actively e?uxing anticancer drugs. (scirp.org)
  • Function of the ABC transporters, P-glycoprotein, multidrug resistance protein and breast cancer resistance protein, in minimal residual disease in acute myeloid leukemia. (vu.nl)
  • ABC-transporters P-glycoprotein (Pgp) and multidrug resistance protein (MRP), are thought to contribute to treatment failure, while it is unknown whether breast cancer resistance protein (BCRP) does so. (vu.nl)
  • Fingerprint Dive into the research topics of 'Function of the ABC transporters, P-glycoprotein, multidrug resistance protein and breast cancer resistance protein, in minimal residual disease in acute myeloid leukemia. (vu.nl)
  • MCF-7/AdrVp is a multidrug-resistant human breast cancer subline that displays an ATP-dependent reduction in the intracellular accumulation of anthracycline anticancer drugs in the absence of overexpression of known multidrug resistance transporters such as P glycoprotein or the multidrug resistance protein. (pnas.org)
  • The mRNA encodes a 663-aa member of the ATP-binding cassette superfamily of transporters that we term breast cancer resistance protein (BCRP). (pnas.org)
  • Upregulation of drug efflux pumps belonging to the family of ATP-binding cassette (ABC) transporters can confer loss of efficacy/resistance to muliple cytostatic drugs, a phenotype referred to as multidrug resistance (MDR). (biomedcentral.com)
  • The adenosine triphosphate (ATP) binding-cassette (ABC) transporters are a superfamily of cellular proteins that have been partly implicated as a cause of multidrug resistance (MDR) in cancer cells. (elsevier.com)
  • It is of great challenge to predict human brain penetration for substrates of multidrug resistance protein 1 (MDR1) and/or breast cancer resistance protein (BCRP), two major efflux transporters at blo. (bioportfolio.com)
  • Multidrug resistance-associated protein 2 (MRP2) also called canalicular multispecific organic anion transporter 1 (cMOAT) or ATP-binding cassette sub-family C member 2 (ABCC2) is a protein that in humans is encoded by the ABCC2 gene. (wikipedia.org)
  • The human multidrug resistance protein (MRP) family contains at least six members: MRP1, the godfather of the family and well known as the multidrug resistance protein, and five homologs, called MRP2-6. (nih.gov)
  • Multidrug resistance-associated protein 2 (MRP2/ABCC2) is mainly expressed in the apical phase of barrier membranes. (springer.com)
  • MRP2/ABCC2 is a member of the integral membrane protein family whose high-resolution crystal structure has not been described. (springer.com)
  • To overcome the obstacle of lacking detailed structural depiction, various molecular modeling approaches have been applied to derive the structural requirements for binding interactions with MRP2/ABCC2 protein, including two-dimensional (2D) and three-dimensional (3D) quantitative SAR (QSAR) analysis, pharmacophore models, and homology modeling of the transporter. (springer.com)
  • Gerk PM, Vore M. Regulation of expression of the multidrug resistance-associated protein 2 (MRP2) and its role in drug disposition. (springer.com)
  • Konig J, Nies AT, Cui Y, Leier I, Keppler D. Conjugate export pumps of the multidrug resistance protein (MRP) family: localization, substrate specificity, and MRP2-mediated drug resistance. (springer.com)
  • b ) reversal of MTX resistance by probenecid in both transfectants, and ( c ) ATP-dependent uptake of [ 3 H]MTX in inside-out vesicles of MRP1 and MRP2 transfectants. (aacrjournals.org)
  • We show here that stable transfection of MRP1 and MRP2 cDNA confers a marked resistance to polyglutamatable antifolate drugs, including MTX, GW1843, and ZD1694. (aacrjournals.org)
  • The human multidrug resistance protein MRP1 and its homolog, MRP2, are both suggested as being involved in cancer drug resistance and the transport of organic anions. (aspetjournals.org)
  • Methotrexate was actively transported by both proteins, although more efficiently by MRP2. (aspetjournals.org)
  • In this study, we investigated the effect of lapatinib on multidrug resistance-associated protein 1 (MRP1 (ABCC1)), MRP2 (ABCC2), MRP4 (ABCC4) and lung relative resistance protein (LRP) drug efflux pumps. (springer.com)
  • To elucidate the role of the multidrug resistance-associated protein (Mrp)-2 in the interaction between MMF and CsA, we treated three groups of 10 Mrp2-deficient rats (TR- rat) for 6 days with either vehicle, CsA (8 mg/kg) or Tac (4 mg/kg) by oral gavage. (eur.nl)
  • The intestinal transport kinetics of CPT were characterized using Caco-2 cells, MDCKII wild-type cells and MDCKII cells transfected with human P-glycoprotein (PGP) (ABCB1) or human multidrug resistance protein 2 (MRP2) (ABCC2). (biomedcentral.com)
  • However, the decrease in the efflux ratio of CPT in MDCKII/MRP2 cells (2.31 to 1.03) suggests that CPT efflux was completely inhibited by MK571, a potent inhibitor of the Multidrug Resistance Protein transporter family. (biomedcentral.com)
  • The role of protein synthesis and degradation in the post-transcriptional regulation of rat multidrug resistance-associated protein 2 (Mrp2, Abcc2). (semanticscholar.org)
  • Multidrug resistance-associated protein 2 (Mrp2, Abcc2), an organic anion transporter present in the apical membrane of hepatocytes, renal epithelial cells, and enterocytes, is postulated to undergo post-transcriptional regulation. (semanticscholar.org)
  • We hypothesized that Mrp2 protein undergoes altered rates of protein synthesis or degradation consistent with different Mrp2 protein expression. (semanticscholar.org)
  • Absolute difference of hepatobiliary transporter multidrug resistance-associated protein (MRP2/Mrp2) in liver tissues and isolated hepatocytes from rat, dog, monkey, and human. (semanticscholar.org)
  • Human contains 49 ATP-binding cassette (ABC) transporter genes and the multidrug resistance associated proteins (MRP1/ABCC1, MRP2/ABCC2, MRP3/ABCC3, MRP4/ABCC4, MRP5/ABCC5, MRP6/ABCC6, MRP7/ABCC10, MRP8/ABCC11 and MRP9/ABCC12) belong to the ABCC family which contains 13 members. (eurekaselect.com)
  • MRP10/ABCC13 is clearly a pseudo-gene which encodes a truncated protein that is highly expressed in fetal human liver with the highest similarity to MRP2/ABCC2 but without transporting activity. (eurekaselect.com)
  • Potential factors for MDR includes enhanced drug detoxification, decreased drug uptake, increased intracellular nucleophiles levels, enhanced repair of drug induced DNA damage, overexpression of drug transporter such as P-glycoprotein(P-gp), multidrug resistance-associated proteins (MRP1, MRP2), and breast cancer resistance protein (BCRP). (frontiersin.org)
  • Multidrug resistance protein 2 (MRP2), encoded by the ATP-binding cassette C2 (ABCC2) gene, is an efflux pump located on the apical membrane of many polarized cells, which transports conjugate compounds by an ATP-dependent mechanism. (upm.edu.my)
  • P-gp and MRP2 play a relevant role for detoxification, thus protecting tubule cells against potential carcinogens, but are also believed to contribute to chemotherapy resistance. (nature.com)
  • P-gp is encoded by the ABCB1 (multidrug resistance protein 1 (MDR1)) gene, localized on chromosome 7q21, and MRP2 by the ABCC2 gene, localized on chromosome 10q23-24. (nature.com)
  • Previous studies with mutant transport-deficient rats (TR(-)), in which the multidrug resistance protein 2 (Mrp2) is lacking, have emphasized the importance of this transport protein in the biliary excretion of a wide variety of glutathione conjugates, glucuronides, and other organic anions. (ru.nl)
  • The MRP1 gene maps to chromosome 16p13.1 and encodes for a protein of 1,531 amino acids. (springer.com)
  • p>This section provides information about the protein and gene name(s) and synonym(s) and about the organism that is the source of the protein sequence. (uniprot.org)
  • This superfamily includes the well characterized periplasmic binding protein-dependent uptake systems of prokaryotes, bacterial exporters, and eukaryotic proteins including the P-glycoprotein associated with multidrug resistance in tumours (MDR), the STE6 gene product that mediates export of yeast a-factor mating pheromone, pfMDR that is implicated in chloroquine resistance of the malarial parasite, and the product of the cystic fibrosis gene (CFTR). (nih.gov)
  • Multidrug resistance protein gene expression in Trichoplusia ni caterpillars. (gc.ca)
  • Only limited increases were detected in a single gene, trnMDR2 , which is the most weakly expressed of the three MDR genes, suggesting that increased multidrug resistance of this type is not a significant part of the response to deltamethrin exposure. (gc.ca)
  • Expression of the multidrug resistance-associated protein (MRP) gene in human cancers. (aacrjournals.org)
  • We determined the expression of a newly recognized drug resistance gene, the multidrug resistance-associated protein (MRP) gene, [Cole et al. (aacrjournals.org)
  • BCRP, encoded by the mxr gene, is a 655-amino acid, 72-kDa protein with a N-terminal ATP-binding site and six transmembrane domains. (aacrjournals.org)
  • The complementary DNA for rat c moat , a homolog of the human multidrug resistance gene (h MRP1 ), was isolated and shown to be expressed in the canalicular membrane of hepatocytes. (sciencemag.org)
  • In the TR − rat, a single-nucleotide deletion in this gene resulted in a reduced messenger RNA level and absence of the protein. (sciencemag.org)
  • In conclusion, our study reveals that the Pfmrp2 gene is the most diverse ABC transporter known in P. falciparum with a potential role in antimalarial drug resistance. (ntu.edu.sg)
  • The protein encoded by this gene is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. (nih.gov)
  • Mutations in this gene are associated with colchicine resistance and Inflammatory bowel disease 13. (nih.gov)
  • Disruption of the PA2491 gene in a mini-Tn 5 - tet insertion mutant of a clinical isolate of Pseudomonas aeruginosa increased expression of the mexEF-oprN multidrug efflux genes and decreased production of outer membrane protein OprD, concomitant with enhanced resistance to chloramphenicol, quinolones, and imipenem, which was reminiscent of previously described nfxC mutants. (asm.org)
  • Association of the multidrug-resistance-associated protein gene (ABCC2) variants with intrahepatic cholestasis of pregnancy. (cdc.gov)
  • To determine the expression of multidrug resistance-associated protein (MRP) gene and its role in gastric and colon cancers, we analyzed 10 gastric and 10 colon non-drug-selected cell lines and a similar number of tissue samples of these cancers. (nebraska.edu)
  • This protein has an unusually broad substrate specificity and is capable of transporting not only a wide variety of neutral hydrophobic compounds, like the MDR1/P-glycoprotein, but also facilitating the extrusion of numerous glutathione, glucuronate, and sulfate conjugates. (springer.com)
  • To determine the frequency and clinical significance of MDR1, MRP1, and LRP in younger AML patients, we developed multiparameter flow cytometric assays to quantify expression of these proteins in pretreatment leukemic blasts from 352 newly diagnosed AML patients (median age, 44 years) registered to a single clinical trial (SWOG 8600). (uni-bonn.de)
  • The activity of P-glycoprotein (Pgp/MDR1/ABCB1) and multidrug resistance proteins (MRP/ABCC) influence the pharmacokinetics and bioavailability of many drugs. (ru.nl)
  • In tissue samples, the expression pattern of the two multidrug resistance (MDR) genes was broadly similar to that described for the cell lines, except that most of the gastric cancer tissue samples did express low levels of mdr1. (nebraska.edu)
  • The ABCB1 transporter (multidrug resistance protein (MDR) p-glycoprotein), expression and function are controlled by hyaluronic acid (HA) and the HA receptor CD44, both of which are altered in primary open angle glaucoma (POAG). (arvojournals.org)
  • These transport properties of MRP1 are responsible for the drug resistance in MRP1-overexpressing cancers that do not express ABCB1 or ABCG2. (springer.com)
  • ABCB1 and ABCC2 mRNA and protein expression levels were determined by real-time polymerase chain reaction or immunohistochemistry in kidney cancer and adjacent unaffected cortex tissue of 82 nephrectomized renal cell cancer (RCC) patients (63 clear-cell RCC (CCRCC), 19 non-CCRCC). (nature.com)
  • T. ABCB1 and ABCC2 were less expressed in CCRCC than in normal cortex on mRNA as well as on protein level. (nature.com)
  • Overexpression of ATP-binding cassette transport proteins, including P-glycoprotein (Pgp), multidrug resistance (MDR) protein (MRP-1), and breast cancer resistance protein (BCRP), is a well-characterized mechanism of MDR in tumor cells. (aacrjournals.org)
  • BCRP protein with an arginine-to-threonine mutation at amino acid 482 (BCRP-T482) confers resistance to anthracyclines, whereas the wild-type protein (BCRP-R482) confers resistance to mitoxantrone but not to anthracyclines ( 8 ). (aacrjournals.org)
  • Intestinal breast cancer resistance protein (BCRP)/Bcrp1 and multidrug resistance protein 3 (MRP3)/Mrp3 are involved in the pharmacokinetics of resveratrol. (semanticscholar.org)
  • Factors that regulate expression of the MRP-related proteins and ABCG2/BCRP are also reviewed. (eurekaselect.com)
  • The prognostic value of Pgp and MRP is, therefore, likely related to drug efflux capacity homogeneously distributed in the whole blast population, while BCRP probably has a limited function in drug efflux-related resistance in AML. (vu.nl)
  • Enforced expression of the full-length BCRP cDNA in MCF-7 breast cancer cells confers resistance to mitoxantrone, doxorubicin, and daunorubicin, reduces daunorubicin accumulation and retention, and causes an ATP-dependent enhancement of the efflux of rhodamine 123 in the cloned transfected cells. (pnas.org)
  • BCRP is a xenobiotic transporter that appears to play a major role in the multidrug resistance phenotype of MCF-7/AdrVp human breast cancer cells. (pnas.org)
  • Downregulation of cytokeratin 18 enhances BCRP-mediated multidrug resistance through induction of epithelial-mesenchymal transition and predicts poor prognosis in breast cancer. (bioportfolio.com)
  • In the present study, we revealed that the expression of CK18 was significantly downregulated in breast cancer tissues and in an MDR cell line overexpressing breast cancer resistant protein (BCRP), and the presence of low levels of CK18 was associated with TNM stage, lymph node metastasis, and unfavorable survival in breast cancer patients. (bioportfolio.com)
  • β-Casein micelles for oral delivery of SN-38 and elacridar to overcome BCRP-mediated multidrug resistance in gastric cancer. (bioportfolio.com)
  • Ex vivo resistance in childhood acute lymphoblastic leukemia: Correlations between BCRP, MRP1, MRP4 and MRP5 ABC transporter expression and intracellular methotrexate polyglutamate accumulation. (bioportfolio.com)
  • Furthermore, these data suggest a mechanism tying accumulation of p53 mutations to the multidrug resistance phenotype seen in this disease. (jci.org)
  • The resistance phenotype is predominantly observed after short-term ( i.e. , clinically relevant) drug exposure, which does not provide sufficient time to convert these drugs into long-chain polyglutamate forms. (aacrjournals.org)
  • Despite comprehensive knowledge on in vitro mechanisms of drug resistance, the precise nature of this in vivo MDR phenotype in breast cancer is still unclear. (aacrjournals.org)
  • These findings led to the hypothesis that an ATP-dependent xenobiotic transporter may contribute significantly to the multidrug-resistance phenotype of MCF-7/AdrVp cells. (pnas.org)
  • Preclinical studies have indicated that resistance to topo-IIalpha drugs depends on topo-IIalpha content and/or activity, the altered-topo-II multidrug resistance phenotype (at-MDR) and/or one of two different drug efflux pumps, P-glycoprotein (P-gp) and the multidrug resistance protein (MRP). (paperity.org)
  • For example, lower levels of taxol resistance are associated with overexpression of MRP than with overexpression of P-glycoprotein. (nih.gov)
  • Overexpression of proteins in this class by NEOPLASMS is considered a possible mechanism in the development of multidrug resistance (DRUG RESISTANCE, MULTIPLE). (curehunter.com)
  • One of the mechanisms capable of contributing to resistance is the overexpression of multidrug resistance (MDR) transporter proteins. (gc.ca)
  • MDR frequently results from overexpression of cell membrane proteins belonging to the ATP-binding cassette (ABC) superfamily, which function as energy-dependent drug efflux pumps. (aacrjournals.org)
  • Studies have linked overexpression of MRP1 with multidrug resistance in cancers of the breast, lung, and prostate. (medicalnewstoday.com)
  • Multidrug resistance proteins (MRPs, ABCCs): importance for pathophysiology and drug therapy. (ebi.ac.uk)
  • Multidrug resistance proteins (MRPs/ABCCs) in cancer chemotherapy and genetic diseases. (ebi.ac.uk)
  • Several MRP/ABCC members (MRPs 1-3) are associated with tumor resistance which is often caused by an increased efflux and decreased intracellular accumulation of natural product anticancer drugs and other anticancer agents. (eurekaselect.com)
  • Click on genes, proteins and metabolites below to link to respective articles. (wikipedia.org)
  • The expression of several drug-resistance genes, including MRP and p53 , increases with advancing stage of human prostate cancer. (jci.org)
  • The aim of this study was to investigate whether expression of particular drug resistance genes in primary operable breast cancer correlates with response to first-line chemotherapy in advanced disease. (aacrjournals.org)
  • For each of these drug resistance genes, a large variation in expression level was observed among the tumors of the different patients. (aacrjournals.org)
  • When analyzing mRNA expression in relation to overall response, it was found that the median expression level of these five drug resistance genes in the responding tumors, as compared with nonresponding tumors, was markedly lower. (aacrjournals.org)
  • Although similar differences in response rate were found for subsets of tumors stratified by the expression level of the other drug resistance genes, none of the observed differences were statistically significant. (aacrjournals.org)
  • Furthermore, no correlation between the expression level of these drug resistance genes and post-relapse overall survival was found. (aacrjournals.org)
  • The multidrug resistance-encoding IncA/C conjugative plasmids disseminate antibiotic resistance genes among clinically relevant enteric bacteria. (edu.au)
  • This enables the EES to encompass mosquito collection and identification, salivary gland DNA extraction, Plasmodium- and species-specific identification, molecular marker-based PCR detection methods for putative drug resistance genes, and data management. (hindawi.com)
  • Both MRP and p-glycoprotein belong to the ATP-binding cassette superfamily of transmembrane transport proteins, but they share only 15% amino acid identity. (nih.gov)
  • The ATP-binding cassette (ABC) superfamily of transport systems now includes over thirty proteins that share extensive sequence similarity and domain organization. (nih.gov)
  • MRP1 belongs to the superfamily of ATP binding cassette transporter proteins (4) and mediates the ATP-driven unidirectional transport of a broad range of neutral as well as anionic compounds across cellular membranes. (aacrjournals.org)
  • Multidrug resistance-associated protein 1 (MRP1) is a member of the ATP-binding cassette membrane transport superfamily and is responsible for multidrug resistance in cancer cells. (nih.gov)
  • Although P-gp and MRP1 have many functional similarities and are both members of the ATP-binding cassette superfamily of proteins, they possess only a 15% amino acid homology ( Cole and Deeley, 1998 ). (aspetjournals.org)
  • Several members of different families of the ATP-binding cassette (ABC) superfamily of transport proteins are capable of transporting an extraordinarily structurally diverse array of endo- and xenobiotics and their metabolites across cell membranes. (eurekaselect.com)
  • Multidrug resistance protein 4 (MRP4) is a member of subfamily C of the ATP-binding cassette superfamily of membrane transport proteins. (oatd.org)
  • The ABC superfamily consists of P-glycoprotein, multidrug resistance-associated proteins (MRP) and breast cancer-related proteins, of which MRP is of particular interest because of its ability to efflux a broader range of substrates. (elsevier.com)
  • Multidrug resistance (MDR) is a major impediment to successful chemotherapy of cancer. (springer.com)
  • Inherent or acquired resistance to multiple natural product drugs is a major obstacle to the success of chemotherapy. (nih.gov)
  • Tumor cell resistance to a wide spectrum of anticancer agents continues to be a major obstacle to curative cancer chemotherapy. (aacrjournals.org)
  • Although MRP1 expression is most often associated with multidrug resistance to cancer chemotherapy agents, antiretroviral agents used in the treatment of human immunodeficiency virus-1 (HIV-1) infection may also interact with these proteins. (aspetjournals.org)
  • Chemotherapy resistance is the major reason for the failure of ovarian cancer treatment. (muni.cz)
  • Despite advances in the field of cancer chemotherapy, drug resistance remains a major problem. (aacrjournals.org)
  • Unfortunately, the occurrence of multidrug resistance (MDR) limits the application of chemotherapy. (springer.com)
  • Multidrug resistance proteins do not predict benefit of adjuvant chemotherapy in patients with completely resected non-small cell lung cancer: International Adjuvant Lung Cancer Trial Biologic Program. (inserm.fr)
  • Different mechanisms in cancer cells become resistant to one or more chemotherapeutics is known as multidrug resistance (MDR) which hinders chemotherapy efficacy. (frontiersin.org)
  • Selective nanocarrier targeting to tumor overcomes dose-limiting side effects, lack of selectivity, tissue toxicity, limited drug access to tumor tissues, high drug doses, and emergence of multiple drug resistance with conventional or combination chemotherapy. (frontiersin.org)
  • Tumor heterogeneity and tumor cell resistance to anticancer drugs thus remains key formidable challenges for effective targeting of drug delivery systems for successful chemotherapy. (frontiersin.org)
  • The main cause of failure in chemotherapy treatments is that tumors develop resistance to anticancer drugs. (medicalnewstoday.com)
  • Cancer cells that develop resistance to chemotherapy drugs often overexpress, or overproduce, transporter proteins. (medicalnewstoday.com)
  • Around 90% of chemotherapy treatment failures are due to acquired drug resistance. (medicalnewstoday.com)
  • A variety of carotenoids induce reduce resistance to chemotherapy in multidrug resistant lymphoma and human breast cancer cell lines. (greenmedinfo.com)
  • Their role in RCC cancer susceptibility or chemotherapy resistance needs further elucidation. (nature.com)
  • These neoplasms originate mostly from mutant epithelial proximal tubule cells, rarely from collecting duct cells and are characterized by lack of early warning signs and relatively strong resistance against radiotherapy and chemotherapy. (nature.com)
  • Multidrug resistance (MDR) is a common problem when fighting cancer with chemotherapy. (muni.cz)
  • BACKGROUND: Multidrug resistance (MDR) is extremely common in hepatocellular carcinoma (HCC) and is a major problem in cancer eradication by limiting the efficacy of chemotherapy. (biomedsearch.com)
  • The presence of MK571 (inhibitor of MRP1 and multidrug resistance protein 4 (MRP4) led to an enhanced effect of vincristine and etoposide in reducing cell viability over a 72 h period. (frontiersin.org)
  • METHODS: Eighty-four radical prostatectomy specimens from patients with localized prostate cancer (PC) (22 neoadjuvant androgen ablation, AA, 62 no AA), 42 non-cancer and 16 advanced PCs were assessed for MRP4/ABCC4 mRNA/protein expression. (garvan.org.au)
  • RESULTS: MRP4/ABCC4 mRNA/protein levels were higher in localized PC compared to non-cancer (P = 0.006). (garvan.org.au)
  • MRP4/ABCC4 protein levels increased in LNCaP cells after DHT which was partially blocked by bicalutamide. (garvan.org.au)
  • To gain insight into mechanisms regulating MRP4 plasma membrane trafficking, its interactions with the PDZ domain-containing CortBP1, a member of Shank2 family of adapter proteins, were investigated. (oatd.org)
  • Since CortBP1 is known to recruit proteins involved in endocytosis, it was hypothesized that CortBP1 plays a role in MRP4 internalization from the plasma membrane. (oatd.org)
  • They also suggested that MRP4 may exist in a complex with CortBP1 and endocytic proteins. (oatd.org)
  • ATP-binding cassette (ABC) transporter proteins are known to cause multidrug resistance in a large range of organisms, including the Apicomplexa parasites. (ntu.edu.sg)
  • Drug transporter proteins drive the cell processes that absorb, distribute, and expel drugs from the body. (medicalnewstoday.com)
  • Two transmembrane xenobiotic transporter proteins, P glycoprotein (Pgp) and the multidrug resistance protein (MRP), cause multidrug resistance when transfected into drug-sensitive cells in culture ( 1 - 5 ). (pnas.org)
  • To accomplish this, they utilize different transporter proteins in their cell membranes, most of which are powered by what is called the proton motive force . (techfragments.com)
  • It belongs to the MRP (multidrug resistance protein) subfamily of the ATP-binding cassette (ABC) transporter family [ PMID: 21103974 ]. (ebi.ac.uk)
  • More specifically, this protein is a member of the MRP subfamily, which is involved in multi-drug resistance. (wikipedia.org)
  • This protein is a member of the MDR/TAP subfamily. (nih.gov)
  • Members of the MDR/TAP subfamily are involved in multidrug resistance. (nih.gov)
  • Confers resistance to anticancer drugs. (drugbank.ca)
  • The human multidrug resistance-associated protein MRP confers resistance to various cytotoxic drugs by lowering the intracellular drug concentration. (jci.org)
  • In this review, we summarize what is known about the protein structure, the expression in tissues, the routing in cells, the physiological functions, the substrate specificity, and the role in multidrug resistance of the individual members of the MRP family. (nih.gov)
  • This change in MRP1 expression was also seen in isogenic cell lines in which p53 was inactivated by human papilloma virus (HPV)16E6 protein or by a dominant-negative mutant. (jci.org)
  • Although several studies have examined the expression of these proteins within the brain barriers (i.e., the blood-brain barrier and choroid plexus), little information is available with respect to brain parenchyma cells such as microglia and astrocytes. (aspetjournals.org)
  • Nonetheless, expression of either protein is associated with reduced drug accumulation within cells and with the development of drug resistance ( Cole and Deeley, 1998 ). (aspetjournals.org)
  • Increased expression of the multidrug resistance protein 1(MRP1) in high grade glioma, and it's role in BBB active transport, highlights this member of the ABC transporter family as a target for improving drug responses in GBM. (frontiersin.org)
  • P-glycoprotein (P-gp) and the multidrug resistance-associated proteins (MRP), whose expression is associated with multidrug resistance, have been recently located in the brain capillary endothelial cells (BCEC) forming the blood-brain barrier (BBB), without taking into account a possible influence or contribution of glial cells and pericytes. (archives-ouvertes.fr)
  • However, lapatinib did not alter the protein or mRNA expression levels of MRP1. (springer.com)
  • The aim of this study was to assess the influence of membrane transporter protein expression on chemotherapeutic response. (archbronconeumol.org)
  • encoding P-glycoprotein) and more recently with expression of other novel proteins conferring multidrug resistance such as MRP1 (multidrug resistance-associated protein 1) and LRP (lung resistance protein). (uni-bonn.de)
  • Protein expression was further correlated with functional efflux by leukemic blasts [assessed using two substrates: Di(OC)(2) and Rhodamine 123] and with the ability of MDR-reversing agents to inhibit efflux in vitro. (uni-bonn.de)
  • Flow Cytometric Assessment of P-glycoprotein and Multidrug Resistance-associated Protein Activity and Expression in Canine Lymphoma. (creativebiomart.net)
  • Involvement of the multidrug resistance protein 3 in drug sensitivity and its expression in human glioma. (semanticscholar.org)
  • Modulation of expression and activity of intestinal multidrug resistance-associated protein 2 by xenobiotics. (semanticscholar.org)
  • Consequences of bile duct obstruction on intestinal expression and function of multidrug resistance-associated protein 2. (semanticscholar.org)
  • Co-expression of oppositely orientated proteins almost exclusively yields antiparallel dimers. (diva-portal.org)
  • Silybin counteracts doxorubicin resistance by inhibiting GLUT1 expression. (greenmedinfo.com)
  • Wogonin decreased the expression of glycolysis-related proteins, glucose uptake and lactate generation in a dose-dependent manner. (greenmedinfo.com)
  • SSZ-resistant cell lines, as well as macrophages from RA patients and healthy controls, were characterized for expression of MDR proteins. (biomedcentral.com)
  • Immunohistochemical studies revealed increased expression of MDR proteins in macrophages from RA patients as compared with controls. (biomedcentral.com)
  • nfxC mutants display resistance to fluoroquinolones, chloramphenicol, trimethoprim, and the carbapenem imipenem ( 14 , 32 ), although resistance to imipenem results not from MexEF-OprN expression ( 32 ) but from the concomitant decrease in outer membrane protein OprD in these mutants ( 14 , 42 ). (asm.org)
  • Flow cytometry was used to analyze the cell cycle distribution and to measure the expression levels of P-glycoprotein (P-gp) and MDR-related protein (MRP)-1 in these cells. (biomedsearch.com)
  • MRP5 could confer resistance to several anticancer drugs, including cisplatin, purine analogues (such as 6-mercaptopurine and 6-thioguanine), pyrimidine analogues (such as gemcitabine, cytosine arabinoside (Ara-C) and 5-fluorouracil (5-FU)) , the natural product doxorubicin and to anti-folate drugs (such as MTX), but not to Vinca alkaloids (such as vincristine) [ PMID: 21740521 ]. (ebi.ac.uk)
  • This distinctive feature of this drug pump explained the cross-resistance to a series of structurally and functionally unrelated anticancer agents. (springer.com)
  • Based on currently available preclinical and limited clinical data, it can be expected that modulation of MRP members may represent a useful approach in the management of anticancer and antimicrobial drug resistance and possibly of inflammatory diseases and other diseases. (eurekaselect.com)
  • It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs. (nih.gov)
  • The multidrug resistance protein (MRP) is an ATP-dependent transport protein for organic anions, as well as neutral or positively charged anticancer agents. (elsevier.com)
  • Small multidrug resistance protein (also known as Drug/Metabolite Transporter) is a family of integral membrane proteins that confer drug resistance to a wide range of toxic compounds by removing them for the cells. (wikipedia.org)
  • Multidrug resistance has long been considered to involve one specific ATP-dependent membrane efflux pump, P-glycoprotein (P-gp). (aspetjournals.org)
  • However, over the last decade it has become apparent that cells that do not express P-gp can also be resistant to a variety of structurally unrelated drugs, which suggested the existence of other membrane-bound efflux proteins. (aspetjournals.org)
  • Supplemental Figure 2 - Immunoblot of membrane proteins from HEK293 cells. (aspetjournals.org)
  • One resistance mechanism involves membrane-embedded multidrug efflux pumps that can effectively extrude an array of substrates, including common antibiotics, dyes, and biocides. (asm.org)
  • Membrane-embedded multidrug efflux pumps are a principal component underlying bacterial resistance, as these proteins can export a variety of toxic compounds. (asm.org)
  • Dynamics of four rat liver plasma membrane proteins and polymeric IgA receptor. (semanticscholar.org)
  • The bacterial multidrug transporter EmrE is a dual-topology membrane protein and as such is able to insert into the membrane in two opposite orientations. (diva-portal.org)
  • Using EmrE variants with fixed, opposite orientations in the membrane, we now show that, although the proteins are able to form parallel dimers, an antiparallel organization of the subunits in the dimer is preferred. (diva-portal.org)
  • In order to function accurately, any integral membrane protein needs to be inserted into the cellular membrane where it belongs, and in that particular membrane it has to attain its proper structure and find partners that might be required for proper function. (diva-portal.org)
  • All membrane proteins have evolved to be inserted in a specific overall orientation, so that e.g. substrate-binding parts are exhibited on the 'right side' of the membrane. (diva-portal.org)
  • So, what determines in which way a membrane protein is inserted? (diva-portal.org)
  • Are all membrane proteins inserted just so ? (diva-portal.org)
  • The focus of this thesis is on these fundamental questions: how, and when, is the overall orientation of a membrane protein established? (diva-portal.org)
  • A closer look at the inner membrane proteome of the familiar gram-negative bacterium Escherichia coli revealed a small group of proteins that, oddly enough, seemed to be able to insert into the membrane in two opposite orientations. (diva-portal.org)
  • We could show that these dual-topology membrane proteins are delicately balanced, and that even the slightest manipulations make them adopt a fixed orientation in the membrane. (diva-portal.org)
  • Further, we show that these proteins are topologically malleable until the very last residue has been synthesized, implying interesting questions about the topogenesis of membrane proteins in general. (diva-portal.org)
  • In addition to PDZ domain-containing adapter proteins, N-glycans can regulate the apical membrane localization of some proteins. (oatd.org)
  • In this fashion, the MexA subunit connected MexB and OprM, indicating that MexA is the membrane bridge protein. (rcsb.org)
  • She is a membrane protein biochemist and biophysicist who has recently engaged in drug discovery projects to find inhibitors of proteins that cause multi-drug resistances in cancers and other diseases. (smu.edu)
  • 6 ) selected human breast carcinoma MCF-7 cells for resistance to the anthracycline doxorubicin in the presence of verapamil, an inhibitor of Pgp. (pnas.org)
  • Simvastatin as Inhibitor of Cell Adhesion Mediated Drug Resistance in Patients With Refractory Multiple Myeloma. (bioportfolio.com)
  • Resveratrol mediated cancer cell apoptosis, and modulation of multidrug resistance proteins and metabolic enzymes. (bioportfolio.com)
  • In vitro statins, inhibitors of the HMG-CoA-reductase, have been shown to overcome cell adhesion mediated drug resistance at very low concentrations. (bioportfolio.com)
  • However, whether ascites drives multidrug resistance in ovarian cancer cells awaits elucidation. (muni.cz)
  • Collectively, our findings identify a novel activity for ascites in promoting ovarian cancer multidrug resistance. (muni.cz)
  • Even though breast cancer is often considered as one of the more chemosensitive solid tumors, all initially responsive tumors relapse and develop resistance to a broad spectrum of drugs known as MDR. (aacrjournals.org)
  • PURPOSE: The purpose of our study was to determine whether multidrug resistance proteins (MRP) are of prognostic and/or predictive value in patients who were enrolled into the International Adjuvant Lung Cancer Trial (IALT). (inserm.fr)
  • Cancer is a heterogeneous disease and use of multiple drugs simultaneously can result in drug resistance which is either intrinsic or acquired known as multidrug resistance (MDR). (frontiersin.org)
  • The protein sits in the cell wall and drives a pump that ejects cancer drugs out of the cell. (medicalnewstoday.com)
  • He states that "Several epidemiologic and preclinical studies show the positive effect of vitamin D in reducing cancer risk and progression, but we are the first to discover its interaction with drug transporter protein and its ability to selectively kill drug-resistant cancer cells. (medicalnewstoday.com)
  • Increased cGMP efflux by ABCC5 may be one mechanism whereby cancer cells can develop resistance against endogenous growth control, and also against antineoplastic drugs which are substrates for ABCC5. (scirp.org)
  • Epstein-Barr virus infection may confer multidrug resistance to breast cancer cells. (greenmedinfo.com)
  • Ampelopsin, a compound found within the Japanese Raisin Tree, reverses multidrug resistance in cancer cells. (greenmedinfo.com)
  • Mbuna, J , Kaneta, T & Imasaka, T 2011, ' Rapid determination of multidrug resistance-associated protein in cancer cells by capillary electrophoresis immunoassay ', Journal of Chromatography A , vol. 1218, no. 25, pp. 3923-3927. (elsevier.com)
  • A dominant hindrance towards curative cancer therapy is multidrug resistance (MDR) mediated by ATP-dependent efflux pum. (bioportfolio.com)
  • Multidrug Resistance Protein-4 Influences Aspirin Toxicity in Human Cell Line," Mediators of Inflammation , vol. 2015, Article ID 607957, 9 pages, 2015. (hindawi.com)
  • Two proteins have been shown to cause this type of multidrug resistance in human tumour cells, the 170 kDa P-glycoprotein and the 190 kDa multidrug resistance protein (MRP). (nih.gov)
  • The uppercase characters identify the human protein, i.e. (springer.com)
  • Structural and functional consequences of mutating cysteine residues in the amino terminus of human multidrug resistance-associated protein 1. (nih.gov)
  • Mutation analyses of the two cysteines in human MRP1 revealed that the Cys(7) residue is critical for the MRP1-mediated drug resistance and leukotriene C(4) transport activity. (nih.gov)
  • Basolateral localization and export activity of the human multidrug resistance-associated protein in polarized pig kidney cells. (jci.org)
  • Liu, Y.-P. The Role of E3 Ubiquitin Ligase Cbl Proteins in β-Elemene Reversing Multi-Drug Resistance of Human Gastric Adenocarcinoma Cells. (mdpi.com)
  • Zhang Y, Mu X-D, Li E-Z, Luo Y, Song N, Qu X-J, Hu X-J, Liu Y-P. The Role of E3 Ubiquitin Ligase Cbl Proteins in β-Elemene Reversing Multi-Drug Resistance of Human Gastric Adenocarcinoma Cells. (mdpi.com)
  • Evidence for two interacting ligand binding sites in human multidrug resistance protein 2 (ATP binding cassette C2). (sigmaaldrich.com)
  • Bartosz, G. 2002-03-25 00:00:00 We employed human red blood cells as a model system to check the affinity of MRP1 (Multi-drug Resistance-associated Protein 1) towards fluorescein and a set of its carboxyl derivatives: 5/6-carboxyfluorescein (CF), 2′,7′-bis-(2-carboxyethyl)-5/6-carboxyfluorescein (BCECF) and calcein (CAL). (deepdyve.com)
  • Characterization of drug transport by the human multidrug resistance protein 3 (ABCC3). (semanticscholar.org)
  • Transport of amphipathic anions by human multidrug resistance protein 3. (semanticscholar.org)
  • The purpose is to study the role of multidrug resistance-associated protein 5, MRP5 in drug metabolism in human retinal pigment epithelium (RPE). (technologynetworks.com)
  • The storage for all reagents of the Human multidrug resistance-associated protein,MRP ELISA Kit should be done at temperatures between 2 and 8 degrees Celsius. (antibody-antibodies.com)
  • Recombinant mouse Multidrug resistance protein 3 mus musculus murine Recombinant mouse Multidrug resistance protein 3 detects proteins from variouse species most likely human. (antibody-antibodies.com)
  • In vitro model systems of human T cells and monocytic/macrophage cell lines were used to provoke resistance to the DMARD sulfasalazine (SSZ). (biomedcentral.com)
  • MDR malaria is the heritable and hypermutable property of human malarial parasite populations that can decrease in vitro and in vivo susceptibility to proven antimalarial drugs as they exhibit dose-dependent drug resistance and delayed parasite clearance time in treated patients. (hindawi.com)
  • Of note, the MDR malaria is demonstrated by the ability of heritable and hypermutable human malarial parasite populations that can decrease in vitro and in vivo susceptibility to proven antimalarial drugs as they exhibit dose-dependent drug resistance and delayed parasite clearance time in treated patients. (hindawi.com)
  • Development of SSZ resistance in T cells and monocytic/macrophage cell lines was accompanied by a marked induction of the MDR protein ABCG2. (biomedcentral.com)
  • Alpha-mangostin has great potential to be further developed into a promising modulator of ABCG2 for reversing multidrug resistance. (greenmedinfo.com)
  • Among these is a small multidrug resistance (SMR) efflux protein, consisting of four transmembrane (TM) helices, that functions as an antiparallel dimer. (asm.org)
  • its substrate specificity depends on the amino acid sequence of the protein. (aacrjournals.org)
  • Impaired renal secretion of substrates for the multidrug resistance protein 2 in mutant transport-deficient (TR-) rats. (ru.nl)
  • There also appear to be fundamental differences in the mechanisms by which the two proteins transport chemotherapeutic drugs. (nih.gov)
  • Resistance may be intrinsic or may be induced by exposure to chemotherapeutic agents ( 1 ). (aacrjournals.org)
  • These proteins owned the ability of conferring resistance to chemotherapeutic agents. (springer.com)
  • The development of resistance to multiple chemotherapeutic drugs occurs frequently during the treatment of advanced carcinoma of the breast. (pnas.org)
  • Contribution of multidrug resistance protein MRP5 in control of cyclic guanosine 5'-monophosphate intracellular signaling in anterior pituitary cells. (ebi.ac.uk)
  • therefore, this protein appears to contribute to drug resistance in mammalian cells. (wikipedia.org)
  • The drug cross-resistance profiles of cells that overexpress MRP or P-glycoprotein are similar but not identical. (nih.gov)
  • This study demonstrates that verapamil and a newly synthesized verapamil derivative, NMeOHI(2), behave as apoptogens in multidrug resistance protein 1 (MRP1)-expressing cells. (biomedsearch.com)
  • These results provide strong evidence that the MRP1 protein is both expressed and functional in microglia cells. (aspetjournals.org)
  • Transport of bile acids in multidrug-resistance-protein 3-overexpressing cells co-transfected with the ileal Na+-dependent bile-acid transporter. (semanticscholar.org)
  • Drug resistance mechanism of antineoplastic agents (Table 1 ) and mechanism of MDR in tumor cells is shown in Figure 1 . (frontiersin.org)
  • Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells. (nih.gov)
  • Collateral sensitivity is the " ability of compounds to kill " multidrug-resistant cells but not the parent cells that they came from. (medicalnewstoday.com)
  • Multidrug-resistant cells have become resistant to drugs that differ, not only in structure, but also in the way that they act. (medicalnewstoday.com)
  • Cholesterol derived from LDL acts as a chemosensitizer in multidrug resistant lymphoblastic leukemia cells. (greenmedinfo.com)
  • Of note, SSZ-resistant cells displayed cross-resistance to methotrexate, but showed enhanced sensitivity to glucocorticoids (prednisone, dexamethasone). (biomedcentral.com)
  • Evolutionary malignant resistance of cells to damaging factors as common biological defence mechanism in neoplastic development. (greenmedinfo.com)
  • The MexEF-OprN system is apparently quiescent in wild-type cells, at least under the usual laboratory growth conditions ( 32 ), but it is expressed in nfxC -type multidrug-resistant strains isolated in vitro ( 14 , 32 , 42 ) and in clinics ( 15 , 24 ). (asm.org)
  • JNK1, JNK2, and JNK3 are involved in P-glycoprotein-mediated multidrug resistance of hepatocellular carcinoma cells. (biomedsearch.com)
  • The mechanism is a drug transporter protein called multidrug resistance-associated protein 1 (MRP1). (medicalnewstoday.com)
  • Our work reveals a novel and unique mechanism of drug resistance in CRC. (biomedcentral.com)
  • Identification of the multidrug resistance protein 1 (MRP1, also denoted as ABCC1) in 1992 [ 24 ], and its initial characterization, elucidated that this protein indeed represents an alternative drug pump. (springer.com)
  • Antisense oligonucleotide-mediated suppression of MRP synthesis offers a highly specific alternative approach to circumventing resistance mediated by this novel drug resistance protein. (nih.gov)
  • This report provides a mechanistic basis for resistance to polyglutamatable antifolates through an MRP-mediated drug extrusion. (aacrjournals.org)
  • Probenecid and sulfinpyrazone may therefore be useful lead compounds for the development of clinical reversal agents specific for MRP-mediated drug resistance. (jci.org)
  • Good Morning David, I've done several years of Multi Drug Resistance Protein work. (histosearch.com)
  • CDC-121 Buffalo, NY 14263 -----Original Message----- From: David Grehan [mailto:[email protected]] Hi histolanders, I am trying to locate a good antibody to Multi Drug Resistance Protein that works well on paraffin processed neuroblastoma tumours. (histosearch.com)
  • Mutations and polymorphisms in the bile salt export pump and the multidrug resistance protein 3 associated with drug-induced liver injury. (semanticscholar.org)
  • Drug resistance toward antineoplastic agents is a result of reduction in the effective concentration of drug in the cell prior to its interaction with the target or due to a combination of processes. (frontiersin.org)
  • The main cause of such resistance are efflux pumps, which drive out so much of the drug that the level that remains in the cell is too low be effective. (medicalnewstoday.com)
  • Accordingly, blockade of MRP3 diminishes the effects on drug resistance of PXR. (biomedcentral.com)
  • hence, alternate or additional drug resistance mechanisms operative in this disease have been sought. (pnas.org)
  • Dr. Vogel has over 40 peer-reviewed publications in leading journals and was recently issued a patent on molecules that reverse multi-drug resistance in cancers. (smu.edu)
  • Jansen G, Scheper RJ, Dijkmans BAC: Multidrug resistance proteins in rheumatoid arthritis, role in disease-modifying antirheumatic drug efficacy and inflammatory processes: an overview. (biomedcentral.com)
  • Risk stratification and treatment of ICU-acquired pneumonia caused by multidrug- resistant/extensively drug-resistant/pandrug-resistant bacteria. (bioportfolio.com)
  • But in a study published today in the journal Proceedings of the National Academy of Sciences , UW-Madison biochemistry professor Katherine Henzler-Wildman and collaborators at the Washington University School of Medicine in St. Louis have found that for E. coli's small multidrug resistance transporter, called EmrE, proton and drug movements are not as strictly coupled. (techfragments.com)
  • Bacteria are constantly at war with each other, so maybe it does play a role in drug resistance. (techfragments.com)
  • Since many Candida species have characteristic and different antifungal drug resistance patterns, identifying Candida infections to species level can be useful for patient treatment. (knowthecause.com)
  • The mechanisms of Candida auris anti-fungal drug resistance are not well known- but may be due to mutations of the Erg11, KFS, and ergosterol mutations or by efflux pump activity. (knowthecause.com)
  • Verapamil and its derivative trigger apoptosis through glutathione extrusion by multidrug resistance protein MRP1. (biomedsearch.com)
  • Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs. (ebi.ac.uk)
  • Canalicular multispecific organic anion transporter/multidrug resistance protein 2 mediates low-affinity transport of reduced glutathione. (springer.com)
  • cDNA cloning of the hepatocyte canalicular isoform of the multidrug resistance protein, cMrp, reveals a novel conjugate export pump deficient in hyperbilirubinemic mutant rats. (springer.com)
  • In humans, there are many importers and exporters of bile juice circulation [ 8 ], such as apical sodium-dependent bile acid transporter (ASBT), Na + taurocholate co-transporting polypeptide (NTCP), Multidrug resistance protein (MRP), bile salts export pump (BSEP), and organic solute transporter (OST). (biomedcentral.com)
  • The MexAB-OprM efflux pump of Pseudomonas aeruginosa is central to multidrug resistance of this organism, which infects immunocompromised hospital patients. (rcsb.org)
  • So instead of pumping drugs out to confer resistance, you have the possibility that you could use it to pump drugs in to kill bacteria. (techfragments.com)
  • While it does pump out antibiotics, it is not the main transporter that aids E. coli in antibiotic resistance, and it's possible it has other purposes still undiscovered. (techfragments.com)
  • The emergence of multidrug-resistant (MDR) strains has made treatment of numerous bacterial infections difficult, particularly in diseases like cystic fibrosis (CF) ( 2 - 4 ). (asm.org)
  • These data suggest that PPF may be repurposed as an adjuvant for fosfomycin to treat infections caused by some FosA-producing, multidrug-resistant, Gram-negative pathogens. (asm.org)
  • The resultant multidrug-resistant subline, MCF-7/AdrVp, exhibits marked crossresistance to certain other anthracyclines [daunorubicin and 3′-deamino-3′-(3-cyano-4-morpholinyl) doxorubicin] and to the anthracenedione mitoxantrone but remains sensitive to vinca alkaloids, paclitaxel ( 6 , 7 ), and cis -platin. (pnas.org)
  • The emergence and spread of multidrug resistant (MDR) malaria caused by Plasmodium falciparum or Plasmodium vivax have become increasingly important in the Greater Mekong Subregion (GMS). (hindawi.com)
  • For example, the Greater Mekong Subregion (GMS) countries-comprising Cambodia, Lao People's Democratic Republic, Myanmar, China (Yunnan, China), Thailand, and Vietnam-have been challenging the emergence and spread of multidrug resistant (MDR) falciparum and vivax malaria-as well as artemisinin resistance in P. falciparum and chloroquine resistance in P. vivax -across the international borders within the GMS countries [ 2 - 8 ]. (hindawi.com)
  • Spontaneous multidrug-resistant mutants of the P. aeruginosa clinical isolate hyperexpressing mexEF-oprN and showing reduced production of OprD were readily selected in vitro, and all of them were shown to carry mutations in PA2491, highlighting the probable significance of such mutations as determinants of MexEF-OprN-mediated multidrug resistance in vivo. (asm.org)
  • Closed genome and comparative phylogenetic analysis of the clinical multidrug resistant Shigella sonnei strain 866. (bioportfolio.com)
  • genome and comparative phylogenetic analysis of the clinical multidrug resistant Shigella sonnei strain 866. (bioportfolio.com)
  • Here we present the complete genome of the clinical multidrug resistant (MDR) strain 866, which is highly susceptible to bacteriophage infections. (bioportfolio.com)
  • Multidrug-resistant Citrobacter freundii ST139 co-producing NDM-1 and CMY-152 from China. (bioportfolio.com)
  • Whole-genome sequencing identification of a multidrug-resistant Listeria monocytogenes serotype 1/2a isolated from fresh mixed sausage in southern Brazil. (bioportfolio.com)
  • A previous study performed by our group reported the characterization of a multidrug-resistant isolate of Listeria monocytogenes serotype 1/2a, named Lm16 isolate. (bioportfolio.com)
  • Describe the risk factors and discuss the management of multidrug-resistant (MDR) bacteria responsible for pneumonia among critically ill patients, including methicillin-resistant Staphylococcus aureu. (bioportfolio.com)
  • Clofazimine improves clinical outcomes in multidrug-resistant tuberculosis: a randomized controlled trial. (bioportfolio.com)
  • Three-component multidrug efflux systems of the resistance-nodulation-division (RND) family are prevalent in gram-negative bacteria, in which they contribute significantly to intrinsic and acquired resistance to a range of clinically important antimicrobial agents (i.e., antibiotics and biocides) ( 48 ). (asm.org)
  • FosA proteins confer fosfomycin resistance to Gram-negative pathogens via glutathione-mediated modification of the antibiotic. (asm.org)
  • ABC proteins transport various molecules across extra- and intra-cellular membranes. (wikipedia.org)
  • Blue-native PAGE analyses of intact oligomers and disulfide cross-linking demonstrate that in membranes, the proteins form parallel dimers only if no oppositely orientated partner is present. (diva-portal.org)
  • The proteins that are embedded in the membranes carry out a wide variety of key functions, from nutrient uptake and waste disposal to cellular respiration and communication. (diva-portal.org)
  • Transport proteins located in the basolateral and canalicular membranes have distinctive roles in mediating the translocation of organic compounds and small solutes across the hepatocyte into the canalicular lumen. (depressionofspirits.com)
  • No X-ray crystal structure of ABCC5 has been reported, but molecular models of ABCC5 may be constructed by homology using a known 3D crystal structure of an evolutionary related protein as a template. (scirp.org)
  • A biochemist and leading authority in electron spin resonance spectroscopy, Professor Pia Vogel's research interests include structure, molecular dynamics, and protein-protein interactions of nucleotide binding proteins. (smu.edu)
  • Whether loss of efficacy/resistance to DMARDs and cytostatic drugs share common molecular mechanisms is not known. (biomedcentral.com)
  • In addition to its role in the export of and resistance to antimicrobials, MexEF-OprN also promotes resistance (or tolerance) to organic solvents ( 36 ), dyes ( 16 ), and biocides, such as triclosan ( 8 ). (asm.org)
  • Induction of multidrug resistance protein 3 (mrp3) in vivo is independent of constitutive androstane receptor. (semanticscholar.org)
  • Up-regulation of basolateral multidrug resistance protein 3 (Mrp3) in cholestatic rat liver. (semanticscholar.org)
  • The PXR and multidrug resistance-related protein 3 (MRP3) expressions were examined by western blot, RT-PCR or immunohistochemistry of TMA. (biomedcentral.com)
  • PXR is a potential biomarker for predicting outcome and activates MRP3 transcription by directly binding to its promoter resulting in an increased L-OHP efflux capacity, and resistance to L-OHP or platinum drugs in CRC. (biomedcentral.com)
  • At present, nine MRP proteins ranging in size from 1,325 to 1,545 amino acids have been identified in humans (hMRP1-9). (aspetjournals.org)
  • This entry represents the multidrug resistance-associated protein 5 (MRP5 or ABCC5). (ebi.ac.uk)
  • Candida auris- Recent Emergence of multidrug resistance fungal infection. (knowthecause.com)
  • In this study, we assessed whether inhibition of FosA by sodium phosphonoformate (PPF) (foscarnet), a clinically approved antiviral agent, would reverse fosfomycin resistance in representative Gram-negative pathogens. (asm.org)
  • Structural model of ATP-binding proteins associated with cystic fibrosis, multidrug resistance and bacterial transport. (nih.gov)