Breast cancer resistance protein (BCRP/ABCG2).
Breast cancer resistance protein (BCRP) was identified 7 years ago as the most recent member of ABC drug efflux membrane transporters. It is a 655 amino acid peptide with an ability to extrude a wide variety of chemical compounds from the cells. Today, it is considered as one of three major transporters causing drug resistance in mammalian cells. It is also distributed in epithelia involved in drug disposition with major role in the placenta, liver and intestine. In addition, BCRP is responsible for the "side population" phenotype of stem cells and seems to play a significant role in protection against hypoxia. BCRP inhibitors are currently searched for to overcome drug resistance and to improve the pharmacokinetics, mainly intestinal absorption, of substrate drugs. Mutant BCRP has also been used as a selectable marker in stem cell gene therapy applications.
Staud
Frantisek
F
Department of Pharmacology and Toxicology, Charles University in Prague, Faculty of Pharmacy in Hradec Kralove, Heyrovskeho 1203, Hradec Kralove 50005, Czech Republic. staud@faf.cuni.cz
Pavek
Petr
P
D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000737:chemistry / Q000378:metabolism / Q000502:physiology*; D006801:Humans; D009154:Mutation; D009363:Neoplasm Proteins / Q000737:chemistry / Q000378:metabolism / Q000502:physiology*; D020641:Polymorphism, Single Nucleotide
C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D009363:Neoplasm Proteins