bcrp - publications

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1. Int J Biochem Mol Biol. 2012;3(1):1-27. Epub 2011 Mar 30.

Human ABCG2: structure, function, and its role in multidrug resistance.

Mo W, Zhang JT.

Department of Pharmacology and Toxicology and IU Simon Cancer Center, Indiana
University School of Medicine Indianapolis, IN 46202, USA.

Human ABCG2 is a member of the ATP-binding cassette (ABC) transporter superfamily
and is known to contribute to multidrug resistance (MDR) in cancer chemotherapy.
Among ABC transporters that are known to cause MDR, ABCG2 is particularly
interesting for its potential role in protecting cancer stem cells and its
complex oligomeric structure. Recent studies have also revealed that the
biogenesis of ABCG2 could be modulated by small molecule compounds. These
modulators, upon binding to ABCG2, accelerate the endocytosis and trafficking to
lysosome for degradation and effectively reduce the half-life of ABCG2. Hence,
targeting ABCG2 stability could be a new venue for therapeutic discovery to
sensitize drug resistant human cancers. In this report, we review recent progress
on understanding the structure, function, biogenesis, as well as physiological
and pathophysiological functions of ABCG2.

PMCID: PMC3325772
PMID: 22509477 [PubMed - in process]