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 ...

A - Tilt: 7° - Segments: 1( 35- 54), 2( 77- 99), 3( 106- 129), 4( 136- 152), 5( 174- 193), 6( 326- 347), 7( 364- 385), 8( 440- 461), 9( 462- 483), 10( 543- 567), 11( 581- 603), 12( 970-995), 13(1017-1039), 14(1088-1111), 15(1112-1129), 16(1196-1217), 17(1229-1250 ...

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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

Kit Component:- KN203070G1, MRPS18A gRNA vector 1 in pCas-Guide vector- KN203070G2, MRPS18A gRNA vector 2 in pCas-Guide vector- KN203070D, donor…

MRP8小鼠单克隆抗体[MRP8 7C12/4](ab20220)可与人样本反应并经WB, ELISA, IHC, Flow Cyt实验严格验证，被1篇文献引用。所有产品均提供质保服务，中国75%以上现货。

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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。

Yaragina, Natalia A.. Nedreaas, Kjell Harald. Koloskova, V.P.. Mjanger, Hildegunn. Senneset, Harald. Zuykova, N.V.. Ågotnes, Per. ...

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 ...

Treatment of experimental animals with prototypical enzyme inducers represents a useful tool to characterize the role of different isozymes in drug metabolism and to improve our knowledge on factors regulating their synthesis at the transcriptional level. The effect of model enzyme inducers on phase II (conjugating) enzyme families, including UDP-glucuronosyltransferases and glutathione-S-transferases, has been well characterized in rodent liver. More recently, the effect of inducers on the expression of canalicular multidrug resistance-associated protein 2 (Mrp2) has been focused upon. The identification of a number of conjugated drugs as Mrp2 substrates suggests that both the conjugation and transport systems act coordinately to improve drug elimination from the body. We provide evidence about circumstances resulting in the simultaneous upregulation of phase II enzymes and Mrp2 in hepatic and extrahepatic tissues, most likely involving activation of common nuclear receptors (e.g., FXR, PXR).

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.

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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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is the angle of rotation (in radians) [1].. MRPs have a singuarity at 360 degrees which can be avoided by ensuring the angle of rotation does not exceed 180 degrees, i.e. switching the direction of the rotation when it is past 180 degrees. This function will always return MRPs corresponding to a rotation of less than or equal to 180 degrees.. ...

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 ...

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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 ...