Mdr1 glycoproteins. Medical search. Frequent questions

Multidrug resistance (MDR) is associated with the expression of P-glycoprotein (P-gp), an ATP-dependent transporter which expels anti-cancer drugs from cells. (nih.gov)
P-glycoprotein, the encoded product of the human MDR1 (ABCB1) gene, is of particular clinical relevance in that this transporter has broad substrate specificity, including a variety of structurally divergent drugs in clinical use today. (unibas.ch)
P-glycoprotein (MDR-1) is a well-known transporter that mediates efflux of chemotherapeutic agents from the intracellular milieu and thereby contributes to drug resistance. (rockefeller.edu)
Our first discovery, with my colleagues Igor Roninson and Ira Pastan, was that multidrug-resistant cancers overexpressed a gene that encoded an ATP-dependent transporter, termed P-glycoprotein, MDR1 or ABCB1. (sciencewatch.com)
Im Mittelpunkt der vorliegenden Promotion steht der Auswärtstransport fluoreszierender (C6-NBD-) Lipid-Analoga und endogener Lipide durch das Multidrug Resistance 1 P-Glycoprotein (MDR1 Pgp), das der ATP Binding Cassette (ABC) Transporter Superfamilie angehört. (hu-berlin.de)
Wie Experimente in einer BCRP überexprimierenden EPG85-257-Sublinie nahelegen, ist ausser MDR1 Pgp möglicherweise ebenfalls der ABC Halb-Transporter Breast Cancer Resistance Protein (BCRP) am Transport von C6-NBD-PS und an der verstärkten Exponierung von endogenem PS beteiligt. (hu-berlin.de)
This thesis focuses on outward transport of fluorescent (C6-NBD-) lipid analogs and endogenous lipids by the Multidrug Resistance 1 P-Glycoprotein (MDR1 Pgp), a member of the ATP binding cassette (ABC) transporter superfamily. (hu-berlin.de)
Besides MDR1 Pgp, the ABC half-size transporter Breast Cancer Resistance Protein (BCRP) is possibly also involved in transport of C6-NBD-PS and in increased exposure of endogenous PS, as found in a BCRP overexpressing EPG85-257 subline. (hu-berlin.de)
To study this vectorial transport of organic cations, we constructed a double-transfected Madin-Darby canine kidney strain II (MDCKII) cell line permanently expressing the human organic cation transporter 1 (OCT1, SLC22A1) in the basolateral membrane and MDR1 P-glycoprotein (MDR1 P-gp, ABCB1), an adenosine triphosphate (ATP)-dependent efflux pump for organic cations, in the apical membrane. (nih.gov)
Additionally, MDCKII single transfectants stably expressing OCT1, MDR1 P-gp, or human organic cation transporter 2 (OCT2, SLC22A2) were generated. (nih.gov)
erdafitinib will increase the level or effect of nadolol by P-glycoprotein (MDR1) efflux transporter. (medscape.com)
lasmiditan increases levels of linagliptin by P-glycoprotein (MDR1) efflux transporter. (medscape.com)
carbamazepine decreases levels of berotralstat by P-glycoprotein (MDR1) efflux transporter. (medscape.com)
primidone decreases levels of berotralstat by P-glycoprotein (MDR1) efflux transporter. (medscape.com)
tepotinib will increase the level or effect of berotralstat by P-glycoprotein (MDR1) efflux transporter. (medscape.com)
the human version of the protein encoded by the MDR1 gene), a drug-transporter glycoprotein associated with the cell or plasma membrane (which encloses the cell's cytoplasm) with a wide variety of drug substrates. (thefutureofthings.com)
The researchers concluded that treatment of the drug-resistant tumor cells with low frequency, low intensity AC stimulation in vitro drastically enhances chemotherapeutic efficacy of doxorubicin, a substrate for the MDR1 glycoprotein drug transporter. (thefutureofthings.com)
Further investigation demonstrated that electrical stimulation not only decreases levels of the MDR1 glycoprotein transporter, but also changes the localization of the MDR1 glycoprotein from close to the plasma membrane to the cytosol (the fluid portion of the cytoplasm). (thefutureofthings.com)

The specific MDR1 P-gp inhibitor, zosuquidar trihydrochloride (LY335979), strongly inhibited berberine efflux into the apical compartment. (nih.gov)
P-glycoprotein (P-gp) substrate status of antineoplastic drugs is important because neoplastic cells that express P-gp can actively efflux P-gp substrates, negatively impacting the drug's efficacy. (cliniciansbrief.com)

thus, chemotherapeutics that are P-gp substrates can cause severe adverse reactions in patients with P-gp dysfunction (eg, dogs with multidrug sensitivity gene [ MDR1 ] mutation [also known as ABCB1 -1delta], cats with ABCB1 1930_1931del TC). (cliniciansbrief.com)
MDR1/ABCB1, MRP2/ABCC2, and breast cancer resistance protein (BCRP)/ABCG2 are expressed in the liver and intestine and contribute to the disposition of many drugs. (aspetjournals.org)
First characterization of fish P-glycoprotein (abcb1) substrate specificity using determinations of its ATPase activity and calcein-AM assay with PLHC-1/dox cell line. (irb.hr)

P-glycoprotein/MDR1, multidrug resistance-associated proteins), nuclear receptors (e.g., glucocorticoid nuclear receptor, pregnane xenobiotic nuclear receptor), and other regulatory factors that control pharmacokinetic and pharmacodynamic phenomena during drug biotransformation in disease states. (ccf.org)
[ 8 ] There is usually an increase in multidrug resistance glycoprotein (MDR-1) on the cell surface. (medscape.com)

Interestingly, MDR1 Pgp has been suggested to exhibit an unusually broad substrate specificity. (hu-berlin.de)
Here, the anionic PS was of particular concern, although previously reported not to be an MDR1 Pgp substrate. (hu-berlin.de)
Assessment of verdinexor as a canine P-glycoprotein substrate. (cliniciansbrief.com)

The disposition of digoxin and the influence of the organic anion transporting polypeptide (Oatp)2 inhibitor rifampicin and the P-glycoprotein (P-gp) inhibitor quinidine on its hepatic disposition were examined in the isolated perfused rat liver. (aspetjournals.org)
Verringerung der PS-Exponierung durch einen Inhibitor von MDR1 Pgp deutet auf den Transport von endogenem PS durch MDR1 Pgp hin. (hu-berlin.de)
Reduction of PS exposure by an MDR1 Pgp inhibitor suggests transport of endogenous PS by MDR1 Pgp. (hu-berlin.de)

In a study led by Luca Cucullo and Damir Janigro from the Cleveland Clinic Lerner College of Medicine in Ohio that was recently published by the open access journal, BioMed Central, tumor cells that overexpress the MDR1 gene product were shown to lose their resistance to anti-tumor drugs by electrical stimulation. (thefutureofthings.com)
In vitro , overexpression of the mdr-1 gene product, P-glycoprotein (Pgp), in tumor cells can confer high-level resistance to natural product-derived cytotoxics-anthracyclines, vinca alkaloids, epipodophyllotoxins, and taxanes. (cancer.gov)

Quantitative targeted absolute proteomic analysis of 31 membrane proteins showed that P-glycoprotein (P-gp/mdr1a) protein expression levels were significantly increased in brain capillaries of PTZ (129%), EL (143%), and PHT mice (192%) compared with controls. (aspetjournals.org)
Dogs with the mutation lack a protein (P-glycoprotein) which is responsible for pumping the drugs from the brain. (australian-shepherd-lovers.com)
71 Clusterin is a small heat shock glycoprotein overexpressed in most of the solid tumors, which promotes apoptosis by binding to various molecules such as BAX (BCL2-associated X protein) 72 and signal transducer and activator of transcription (STAT)−1. (oncologynurseadvisor.com)

Juliano, R. L. & Ling, V. A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. (nature.com)
The apparent permeability value for rosuvastatin across MDR1-Madin-Darby canine kidney cells was low (∼8 nm/s), and no directional transport was observed. (aspetjournals.org)

In the present study, MDR1 P-gp was immunodetected by Western blot analysis in 60 human brain tumors, including meningiomas, schwannomas, low-grade gliomas (astrocytomas, pilocytic astrocytomas) and high-grade gliomas (anaplastic astrocytomas, glioblastomas and anaplastic oligodendrogliomas). (nih.gov)
These results indicate that the majority of primary brain tumors express MDR1 P-gp and that its high expression levels in meningiomas may be a marker for this type of brain tumor. (nih.gov)

H19 was also found to induce p-glycoprotein expression and MDR1-associated drug resistance in hepatic carcinoma cells by regulating the demethylation of the MDR1 promoter ( 11 ). (spandidos-publications.com)

What Are The Symptoms Of MDR1 Sensitivity? (australian-shepherd-lovers.com)
There are many possible symptoms associated with the sensitivity to certain drugs caused by the MDR1 gene mutation. (australian-shepherd-lovers.com)
Remember, Imodium (loperamide) is used for the treatment of diarrhea is on the list of drugs that are considered dangerous for dogs with the MDR1 sensitivity. (australian-shepherd-lovers.com)

In a flow cytometry setup, the exposure of endogenous PS on the outer plasma membrane leaflet was significantly elevated in MDR1 overexpressing cells compared to controls. (hu-berlin.de)

Upon intracellular labelling with C6-NBD-PS using a novel approach, significantly increased outward transport of this analog in MDR1 overexpressing cells could be attributed to MDR1 Pgp by employing specific inhibitors. (hu-berlin.de)
When transfected cells were grown polarized on permeable filter supports, berberine was transferred from the basolateral to the apical compartments many times faster by MDCK-OCT1/MDR1 P-gp double transfectants than by MDCK-OCT1 or MDCK-MDR1 P-gp single transfectants. (nih.gov)
Cells that overexpress the MDR1 gene are, hence, resistant to many drugs. (thefutureofthings.com)
The effects of 3, 3', 4, 4', 5-pentachlorobiphenyl (PCB-126), which is the most toxic congener of coplanar polychlorinated biphenyls (Co-PCBs), on intracellular accumulation and transepithelial transport of vinblastine were examined in porcine kidney cells, LLC-PK1, and its transformant cells expressing human P-glycoprotein (LLC-MDR1). (go.jp)
In both cells, the accumulation increased with the addition of PCB-126 and cyclosporine A (CYA), which are P-glycoprotein modulators, though the magnitudes were different in these two cell groups as well as for these two chemicals. (go.jp)

Dogs affected by the MDR1 mutation or with unknown MDR1 status can thus be given verdinexor at labeled doses for treatment of lymphoma. (cliniciansbrief.com)
Think Your Dog Is Safe Because They Tested Negative For MDR1 Gene Mutation? (australian-shepherd-lovers.com)
However, the MDR1 gene mutation can be fatal when affected Aussies are exposed to medications like Trifexis and Ivermectin for dogs (among many other medications). (australian-shepherd-lovers.com)
While this may have been true for those dogs is not true for all Aussies as some have a genetic mutation of the MDR1 gene. (australian-shepherd-lovers.com)
So What Is The MDR1 Gene Mutation And Why Does It Only Affect Certain Dogs? (australian-shepherd-lovers.com)
MDR stands for multi-drug resistance and the mutation in the MDR1 gene prevents many breeds, including Australian Shepherds, from removing many drugs from the brain resulting in toxicity. (australian-shepherd-lovers.com)
The MDR1 mutation is believed to occur in approximately 50% of Australian Shepherds. (australian-shepherd-lovers.com)
Dogs with the MDR1 mutation can be 200 times more sensitive to the drugs than dogs that do not have this mutation. (australian-shepherd-lovers.com)
Since there is such a wide range of symptoms and so many different drugs that can affect dogs with the MDR1 gene mutation it is best to, of course, avoid use of the implicated drugs and to keep a close watch on your dogs for any reaction after administering any medication no matter how seemingly harmless. (australian-shepherd-lovers.com)

4 Bissonnette S, Paradis M, Daneau I, Silversides D. Survey of the MDR1 gene for heterozygous mutations in dogs displaying subchronic toxicity signs to systemic macrocyclic lactones follwing treatment regimen for a genera - lized demodicosis. (thieme-connect.de)

The MDCK-OCT1/MDR1 P-gp double transfectants may be useful to identify additional cationic substrates and inhibitors of OCT1 and MDR1 P-gp, including drug candidates. (nih.gov)

An increasing number of studies have also implicated certain commonly occurring SNPs in MDR1 in problems including altered drug levels and host susceptibility to diseases such as Parkinson's disease, inflammatory bowel disease, refractory seizures, and CD4 cell recovery during human immunodeficiency virus therapy. (unibas.ch)
In this review SNPs in MDR1 in relation to population frequencies, drug levels, and phenotypes are outlined. (unibas.ch)
Ivermectin is not thought to readily cross the blood-brain barrier in humans as it is excluded by a P-glycoprotein drug pump (mdr-1). (drugs.com)
This altered expression of the MDR1 glycoprotein is believed to have caused the loss of the cell's drug extrusion ability, which it mediates. (thefutureofthings.com)

In a human gastric carcinoma cell line (EPG85-257) overexpressing MDR1, outward transport of phosphatidylcholine, phosphatidylethanolamine, glucosylceramide and sphingomyelin analogs via MDR1 Pgp was confirmed using fluorescence spectroscopy. (hu-berlin.de)

Das anionische Lipid PS war hier von besonderem Interesse, obgleich es in vorhergehenden Arbeiten nicht als MDR1 Pgp Substrat betrachtet wurde. (hu-berlin.de)
In addition, decreased accumulation of analogs of diacylglycerol and ceramide suggest MDR1 Pgp mediated transport of these lipid species. (hu-berlin.de)

Transport of C6-NBD-PS was furthermore characterized here in four additional cell lines of different species and tissue origin with varying synthesis levels of MDR1 Pgp. (hu-berlin.de)

A physiologic function for p-glycoprotein (MDR-1) during the migration" by Gwendalyn J. Randolph, Sylvia Beaulieu et al. (rockefeller.edu)

In addition, issues relating to MDR1 haplotypes, environmental factors, and study design, as potential confounding factors of the observed MDR1 polymorphism effect in vivo, are also discussed. (unibas.ch)
The present study was designed to determine whether rosuvastatin is transported by MDR1, MRP2, and BCRP. (aspetjournals.org)

[ 15 , 24 ] More interestingly, results from liver transplant recipients receiving tacrolimus demonstrated that there was a strong correlation between a higher intestinal mRNA expression of the MDR1 gene and the incidence of acute rejection. (medscape.com)
Regarding the clinical impact of the MDR1 gene, the role of the MDR1 donor genotype has been evaluated with reference to the incidence of nephrotoxicity. (medscape.com)
1. UHRF1 inhibits MDR1 gene transcription and sensitizes breast cancer cells to anticancer drugs. (nih.gov)
8. Human AP endonuclease (APE1/Ref-1) and its acetylation regulate YB-1-p300 recruitment and RNA polymerase II loading in the drug-induced activation of multidrug resistance gene MDR1. (nih.gov)
16. Involvement of CtBP1 in the transcriptional activation of the MDR1 gene in human multidrug resistant cancer cells. (nih.gov)
This evidence supports the proposal, now widely accepted, that P-glycoprotein (P-gp), the product of the MDR1 gene, is an energy-dependent pump, ferrying toxins or drugs out of the cell. (nih.gov)
Previous studies by our group have identified a set of genes, including multidrug resistance gene 1 (MDR1), that are regulated by Hh signaling in ovarian cancer. (spandidos-publications.com)
MDR1 is a target gene of the Hh signaling pathway and this pathway may affect chemoresistance of ovarian cancer to DDP via MDR1. (spandidos-publications.com)
The 293T cell was transfected by the retroviral vector PMX-flag-MDR1-GFP together with its peripheral membrane protein gene. (ajol.info)
We successfully observed the expression of the reporter gene-GFP by using the green light fluorescence microscope and the p-glycoprotein (P-gp) expressed by exogenous gene MDR1 by Western Blotting. (ajol.info)
All these facts indicated that the retroviral vector PMX-flag-MDR1-GFP had successfully been transfected into HPMSCs and the exogenous gene multidrug resistance (MDR)1 was detected as normally expressed. (ajol.info)
Effect of risperidone metabolism and P-glycoprotein gene polymorphism on QT interval in patients with schizophrenia. (cdc.gov)
P-glycoprotein (P-gp), encoded by the MDR1 (Multidrug Resistance Protein 1) gene, is an efflux transporter that plays a crucial role in drug disposition. (adaricell.com)
Many Collies have a mutation in the gene making their central nervous system more available to certain drugs than would be the cases in dogs with normal P-glycoprotein. (vin.com)
This study investigated the safety of oral administration of fluralaner at 3 times the highest expected clinical dose to Multi Drug Resistance Protein 1 (MDR1(-/-)) gene defect Collies. (illinois.edu)
Because of the prevalence of the P-glycoprotein gene mutation, genetic testing is recommended for dogs of the following breeds: Collie, Shetland sheepdog, Australian Shepherd, Old English Sheepdog, Long-Haired Whippet, and possibly other herding breeds. (vin.com)

We evaluated alterations in P-gp-mediated transport of anticancer agents due to the MDR1 G1199A polymorphism.Using stable recombinant epithelial cells expressing wild-type (MDR1 (wt)) or G1199A (MDR1 (1199A)), anticancer drug sensitivity and transepithelial permeability were evaluated.The recombinant cells MDR1 (wt) and MDR1 ( 1199A ) displayed comparable doxorubicin resistance. (nih.gov)
Overall, the MDR1 G1199A polymorphism may impact anticancer efficacy through modulation of drug distribution and delivery to target tumor cells. (nih.gov)

In vitro models based on brain capillary endothelial cells (BCECs) are among the most versatile tools in blood-brain barrier research for testing drug penetration into the brain and how this is affected by efflux transporters such as P-glycoprotein (Pgp). (biomedcentral.com)
A 170-kDa transmembrane glycoprotein from the superfamily of ATP-BINDING CASSETTE TRANSPORTERS. (bvsalud.org)
Moreover, there was no difference between influx and efflux amount of TQ in cells with inhibited and non-inhibited MDR1 transporters. (ac.ir)

The primary application of INDIGO Biosciences MDR1 drug interaction assay kit is to rapidly assess drug candidates as either inhibitors, substrates, or non-substrates of P-glycoprotein. (indigobiosciences.com)
In addition, with substitution of MDR1 residues 318-332 (TM6) and 937-994 (TM11-12), MDR2 had relatively normal affinity for MDR1 substrates, but it did not have multidrug transporter activity. (aspetjournals.org)
Reducing Adverse Drug Reactions: Understanding the interaction between a drug and MDR1 can help identify potential adverse reactions, especially in the case of drugs that are substrates for this protein. (adaricell.com)

Significant interindividual variations in the expression and function of P-glycoprotein (P-gp) may be the result of genetic polymorphisms. (medscape.com)
The conclusion lays a solid foundation of the clinical application of MDR1 genetic therapy. (ajol.info)
Certain MDR1 genetic variants are known to compromise the function of this transporter and may thus be associated with Parkinson disease (PD). (uni-luebeck.de)

In all thermoresistant counterparts basal expression of BCRP/MXR, MRP1 and MDR1/PGP was increased relative to thermosensitive sublines. (mdc-berlin.de)

3. Survivin transcription is associated with P-glycoprotein/MDR1 overexpression in the multidrug resistance of MCF-7 breast cancer cells. (nih.gov)
Overexpression of this glycoprotein is associated with multidrug resistance (see DRUG RESISTANCE, MULTIPLE). (bvsalud.org)

MDR1 -EGFP-transduced variants were derived from WT cells by lentiviral transduction, using an MDR1 -linker-EGFP vector. (biomedcentral.com)
MDR1 variants and risk of Parkinson disease: Association with pesticide exposure? (uni-luebeck.de)
We therefore conducted a large case-control study investigating the potential relationship between MDR1 variants and PD. (uni-luebeck.de)
We determined the frequency of three MDR1 variants in 599 European PD patients and controls and further stratified the population by ethnicity, age at onset, and exposure to pesticides. (uni-luebeck.de)
p = 0.047), suggesting that common MDR1 variants might influence the risk to develop PD in conjunction with exposure to pesticides. (uni-luebeck.de)
Dive into the research topics of 'MDR1 variants and risk of Parkinson disease: Association with pesticide exposure? (uni-luebeck.de)

4. Histone methyltransferase MLL1 regulates MDR1 transcription and chemoresistance. (nih.gov)

Lymphocyte homing is mediated by a specific interaction between the lymphocyte homing receptor L-selectin and its sulfated glycoprotein ligands, which are expressed on high endothelial venules (HEV) in the lymph nodes. (go.jp)

As P-glycoprotein can affect drug absorption, distribution, metabolism, and excretion, understanding its interaction with a new drug candidate can be essential. (adaricell.com)
Facilitating Drug Development: Early testing of drug candidates with MDR1 could identify potential issues with drug metabolism and effectiveness, leading to more efficient drug development and reducing the risk of late-stage failure. (adaricell.com)

MDR1/PGP expression was distinctly elevated in the classical MDR subline EPG85-257RDB (vs. parental and atypical MDR sublines). (mdc-berlin.de)
However, compared to freshly isolated brain capillaries or primary BCECs, the expression of Pgp in immortalized BCEC lines is markedly lower, which prompted us previously to transduce the widely used human BCEC line hCMEC/D3 with a doxycycline-inducible MDR1 -EGFP fusion plasmid. (biomedcentral.com)
Compared to WT cells, the MDR1 -EGFP transduced cells exhibited a significantly higher expression and function of Pgp. (biomedcentral.com)
Previous studies revealed that the NNS sucralose (Sucr) altered P-glycoprotein (PGP) expression in rat colon. (mdpi.com)
5. Metformin inhibits P-glycoprotein expression via the NF-κB pathway and CRE transcriptional activity through AMPK activation. (nih.gov)
17. Determining MDR1/P-glycoprotein expression in breast cancer. (nih.gov)
19. Glucosylceramide synthase upregulates MDR1 expression in the regulation of cancer drug resistance through cSrc and beta-catenin signaling. (nih.gov)
HCT-Pgp cells are a proprietary cell line that have been extensively selected for high-level expression of native P-glycoprotein. (indigobiosciences.com)
However, the association between Hh signaling activation and MDR1 expression requires further validation. (spandidos-publications.com)
In the present study, reverse transcription‑quantitative PCR or western blot assays were used to evaluate the mRNA and protein expression levels of MDR1, Sonic Hh (Shh), glioma‑associated oncogene 2 (Gli2), Gli1 and γ‑phosphorylated H2A.X variant histone (γ‑H2AX). (spandidos-publications.com)
Knockdown of Gli2 or targeting the Hh signaling pathway with GANT61 also increased γ‑H2AX levels but decreased the expression of MDR1 in the presence of DDP. (spandidos-publications.com)
MDR1 expression is regulated by the Hh signaling pathway and is likely a downstream transcription factor of Gli2. (spandidos-publications.com)
Modeling of hAβ 40 data after intravenous and intracerebroventricular administration to the rat revealed an initially faster plasma half-life that reflected faster peripheral distribution but slower equilibration between plasma and brain/cerebrospinal fluid even with calcitriol pretreatment that increased P-glycoprotein protein expression and enhanced efflux clearance from brain. (aspetjournals.org)

A ready-to-use monolayer cell-based assay for MDR1 in-vitro evaluation of drug interactions with the P-gp/MDR1 transporter. (adaricell.com)

Sixteen Collies homozygous for the MDR1 deletion mutation were included in the study. (illinois.edu)
Results: No adverse events were observed subsequent to fluralaner treatment of MDR1(-/-) Collies at three times the highest expected clinical dose. (illinois.edu)
Conclusions: Fluralaner chewable tablets are well tolerated in MDR1(-/-) Collies following oral administration. (illinois.edu)

substituting these residues allows the N-terminal transmembrane region of MDR2 to support MDR1 activity. (aspetjournals.org)

The present data indicate that MDR1 -EGFP transduced RBE4 cells are an interesting tool to study the biogenesis of lysosomes and Pgp-mediated lysosomal drug trapping in response to chemotherapeutic agents and other compounds at the level of the blood-brain barrier. (biomedcentral.com)

14. Suppression of αvβ6 downregulates P-glycoprotein and sensitizes multidrug-resistant breast cancer cells to anticancer drugs. (nih.gov)
These results suggest that the inability of MDR2 to transport most MDR1 drugs efficiently may be due to failure of those drugs to stimulate ATPase and activate transport as well as to decreased drug binding. (aspetjournals.org)
However, paradoxically P-glycoprotein overexpressing drug resistant cells are "collaterally sensitive" to non-toxic drugs that stimulate its ATPase activity. (researchsquare.com)
Understanding Drug Interactions: It can be used to understand how drugs interact with the P-glycoprotein (MDR1), a key component of the body's defense mechanism against potentially harmful substances. (adaricell.com)
Understanding how drugs interact with MDR1 can be beneficial in the development of effective treatment strategies. (adaricell.com)
The P-glycoprotein is involved in keeping certain drugs out of certain body tissues (the central nervous system in particular). (vin.com)
P-glycoprotein was stimulated as a function of the concentration with 19 structurally different drugs, including local anesthetics, cyclic peptides, and cytotoxic drugs. (unibas.ch)
In normal patients, the P-glycoprotein is involved in keeping drugs out of certain tissues and is important in keeping milbemycin oxime out of the patient's nervous system. (vin.com)

However, significant differences were observed in the localization of Pgp in that RBE4- MDR1 -EGFP cells expressed Pgp primarily at the plasma membrane, whereas in hCMEC/D3 cells, the Pgp-EGFP fusion protein was visible both at the plasma membrane and in endolysosomal vesicles. (biomedcentral.com)
Multidrug resistance (MDR) mediated by P-glycoprotein (MDR1) is clinically significant. (aspetjournals.org)
Identifying Potential Drug Resistance: MDR1 plays a significant role in multidrug resistance, particularly in cancer treatment. (adaricell.com)

The kinetics of human amyloid-β (hAβ) 40 were examined in the rat pursuant to intravenous and intracerebroventricular administration after pretreatment with calcitriol, the active vitamin D receptor ligand (6.4 nmol·kg −1 in 0.3 ml corn oil every other day for four intraperitoneal doses) to induce P-glycoprotein (P-gp) and enhance hAβ 40 brain efflux. (aspetjournals.org)
A healthy P-glycoprotein system is what allows milbemycin oxime to be safe for mammals even in very high doses. (vin.com)

Although data concerning the outward transport of glucocorticoids from the brain by P-glycoprotein (Pgp) are inconsistent, it has been hypothesized that antidepressants exert their clinical activity in parts by inhibiting Pgp, subsequently leading to enhanced brain glucocorticoid levels and the normalization of the HPA axis function. (nature.com)

15. Reversal of MDR1/P-glycoprotein-mediated multidrug resistance by vector-based RNA interference in vitro and in vivo. (nih.gov)
The result indicates that MDR1 retroviral vector can transfect the HPMSCs. (ajol.info)

To understand P-glycoprotein in more detail, it is important to elucidate its activity in the cellular ensemble as well as in plasma membrane vesicles (under conditions where other ATP dependent proteins are blocked). (unibas.ch)

Concerning tacrolimus and P-gp, some studies found that tacrolimus dose requirement was lower in patients who had one or two mutant alleles in their exon 12, 21, and 26 SNP of MDR1. (medscape.com)

Localization, trafficking, and function of Pgp were compared in WT and MDR1 -EGFP transduced cell lines. (biomedcentral.com)

MDR1-Type P- glycoprotein) may play an important role in drug accumulation and hypersensitivity reactions. (nih.gov)

We found that the N-terminal half of MDR1 and MDR2 was mostly exchangeable except for a few residues in TM6. (aspetjournals.org)
However, this degree of exchangeability was not found in the C-terminal half of MDR1 and MDR2. (aspetjournals.org)
P-glycoprotein (MDR1) efflux transporter found in approximately equal medicine affecting your mouth and throat. (nutshellurl.com)

Anatomy23

Organisms31

Diseases1

Chemicals and Drugs135

Analytical, Diagnostic and Therapeutic Techniques and Equipment22

Phenomena and Processes40

Disciplines and Occupations2

Information Science4

Transporter18

Efflux2

ABCB13

Multidrug2

Substrate3

Inhibitor3

Tumor cells2

Protein3

Permeability2

Tumors2

Hepatic1

Sensitivity3

Plasma membrane1

Cells5

Mutation9

Toxicity1

Inhibitors1

Drug4

Human1

Lipid2

Levels1

Function1

Study2

Gene16

Polymorphism2

Transporters3

Substrates3

Genetic3

BCRP1

Overexpression2

Variants6

Chemoresistance1

Ligands1

Metabolism2

Expression13

Assay1

Collies3

Transmembrane1

Blood-brain b1

Drugs8

Significant3

Doses2

Brain1

Vector2

Plasma1

Patients1

Cell1

Important1

Found3