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Assessment of P-Glycoprotein Substrate and Inhibition Potential of Test Compounds in MDR1-Transfected MDCK Cells.

Curr Protoc Pharmacol. 2012 Sep;Chapter 7:Unit7.13

Authors: C L Lam K, Rajaraman G


P-glycoprotein (P-gp) is the most widely studied drug transporter due to its potential role in drug disposition and efficacy, and drug-drug interactions (DDI). It is abundantly expressed in both the intestinal wall and blood-brain barrier where it serves as a drug permeability barrier while simultaneously facilitating drug elimination in the liver and kidney. It is also abundantly expressed in tumors where it can facilitate the elimination of chemotherapeutics, a phenomenon known as multidrug resistance (MDR). Clinically relevant DDIs involving P-gp are well documented; for example, the P-gp substrate, digoxin, exhibits toxicity when co-administered with a Pgp-inhibitor. This makes it essential to screen new chemical entities early in development for their potential to be a substrate and/or inhibitor of P-gp. Detailed in this unit is an in vitro protocol for assessing the P-gp substrate and inhibition potential of test compounds using the MDCK MDR1 and MDCK WT cell lines. Curr. Protoc. Pharmacol. 58:7.13.1-7.13.17. © 2012 by John Wiley & Sons, Inc.

PMID: 22948850 [PubMed - in process]