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1. Biochem Pharmacol. 2012 Jan 11. [Epub ahead of print]

Role of breast cancer resistance protein (BCRP/ABCG2) in cancer drug resistance.

Natarajan K, Xie Y, Baer MR, Ross DD.

University of Maryland Greenebaum Cancer Center, Baltimore, MD 21201, USA.

Since cloning of the ATP-binding cassette (ABC) family member breast cancer
resistance protein (BCRP/ABCG2) and its characterization as a multidrug
resistance efflux transporter in 1998, BCRP has been the subject of more than two
thousand scholarly articles. In normal tissues, BCRP functions as a defense
mechanism against toxins and xenobiotics, with expression in the gut, bile
canaliculi, placenta, blood-testis and blood-brain barriers facilitating
excretion and limiting absorption of potentially toxic substrate molecules,
including many cancer chemotherapeutic drugs. BCRP also plays a key role in heme
and folate homeostasis, which may help normal cells survive under conditions of
hypoxia. BCRP expression appears to be a characteristic of certain normal tissue
stem cells termed "side population cells," which are identified on flow
cytometric analysis by their ability to exclude Hoechst 33342, a BCRP substrate
fluorescent dye. Hence, BCRP expression may contribute to the natural resistance
and longevity of these normal stem cells. Malignant tissues can exploit the
properties of BCRP to survive hypoxia and to evade exposure to chemotherapeutic
drugs. Evidence is mounting that many cancers display subpopulations of stem
cells that are responsible for tumor self-renewal. Such stem cells frequently
manifest the "side population" phenotype characterized by expression of BCRP and
other ABC transporters. Along with other factors, these transporters may
contribute to the inherent resistance of these neoplasms and their failure to be
cured.

Published by Elsevier Inc.

PMID: 22248732 [PubMed - as supplied by publisher]