P-glycoprotein: from genomics to mechanism

SV Ambudkar, C Kimchi-Sarfaty, ZE Sauna… - Oncogene, 2003 - nature.com
Resistance to chemically different natural product anti-cancer drugs (multidrug resistance, or
MDR) results from decreased drug accumulation, resulting from expression of one or more …

Impact of Genetic Polymorphisms of ABCB1 (MDR1, P-Glycoprotein) on Drug Disposition and Potential Clinical Implications: Update of the Literature

S Wolking, E Schaeffeler, H Lerche, M Schwab… - Clinical …, 2015 - Springer
ATP-binding cassette transporter B1 (ABCB1; P-glycoprotein; multidrug resistance protein 1)
is an adenosine triphosphate (ATP)-dependent efflux transporter located in the plasma …

A "Silent" Polymorphism in the MDR1 Gene Changes Substrate Specificity

C Kimchi-Sarfaty, JM Oh, IW Kim, ZE Sauna… - Science, 2007 - science.org
Synonymous single-nucleotide polymorphisms (SNPs) do not produce altered coding
sequences, and therefore they are not expected to change the function of the protein in …

Polymorphisms in Human MDR1 (P‐glycoprotein): Recent Advances and Clinical Relevance

C Marzolini, E Paus, T Buclin… - Clinical Pharmacology & …, 2004 - Wiley Online Library
Drug transporters are increasingly recognized to be important to drug disposition and
response. P‐glycoprotein, the encoded product of the human MDR1 (ABCB1) gene, is of …

Effect of CYP3A and ABCB1 Single Nucleotide Polymorphisms on the Pharmacokinetics and Pharmacodynamics of Calcineurin Inhibitors: Part I

CE Staatz, LK Goodman, SE Tett - Clinical pharmacokinetics, 2010 - Springer
The calcineurin inhibitors ciclosporin (cyclosporine) and tacrolimus are immunosuppressant
drugs used for the prevention of organ rejection following transplantation. Both agents are …

A synonymous polymorphism in a common MDR1 (ABCB1) haplotype shapes protein function

KL Fung, MM Gottesman - Biochimica et Biophysica Acta (BBA)-Proteins …, 2009 - Elsevier
The MDR1 (ABCB1) gene encodes a membrane-bound transporter that actively effluxes a
wide range of compounds from cells. The overexpression of MDR1 by multidrug-resistant …

Role of pharmacogenetics of ATP-binding cassette transporters in the pharmacokinetics of drugs

I Cascorbi - Pharmacology & therapeutics, 2006 - Elsevier
Interindividual differences of drug response are an important cause of treatment failures and
adverse drug reactions. The identification of polymorphisms explaining distinct phenotypes …

ABCB1 genotype and PGP expression, function and therapeutic drug response: a critical review and recommendations for future research

GD Leschziner, T Andrew, M Pirmohamed… - The …, 2007 - nature.com
The product of the ABCB1 gene, P-glycoprotein (PGP), is a transmembrane active efflux
pump for a variety of drugs. It is a putative mechanism of multidrug resistance in a range of …

The clinical impact of pharmacogenetics on the treatment of epilepsy

W Löscher, U Klotz, F Zimprich, D Schmidt - Epilepsia, 2009 - Wiley Online Library
Drug treatment of epilepsy is characterized by unpredictability of efficacy, adverse drug
reactions, and optimal doses in individual patients, which, at least in part, is a consequence …

Association of the multidrug resistance-1 gene single-nucleotide polymorphisms with the tacrolimus dose requirements in renal transplant recipients

D Anglicheau, P Laurent-Puig… - Journal of the …, 2003 - journals.lww.com
The immunosuppressive drug tacrolimus, whose pharmacokinetic characteristics display
large interindividual variations, is a substrate for P-glycoprotein (P-gp), the product of the …