ABCG2 -- a transporter for all seasons.
The human ABCG2 (ABCP/MXR/BCRP) protein is a recently recognized ABC half-transporter, which forms homodimers in the plasma membrane and actively extrudes a wide variety of chemically unrelated compounds from the cells. This protein protects our cells and tissues against various xenobiotics, with a crucial role in the intestine, liver, placenta, and the blood-brain barrier. Moreover, ABCG2 seems to have a key function in stem cell protection/regulation, and also in hypoxic defense mechanisms. Widely occurring single nucleotide polymorphisms in ABCG2 may affect absorption and distribution, altering the effectiveness and toxicity of drugs in large populations. At the clinics, overexpression of ABCG2 in tumor cells confers cancer multidrug resistance to a variety of newly developed anticancer agents. On the other hand, specific substrate mutants of ABCG2 are advocated for use as selectable markers in stem-cell based gene therapy.
Sarkadi
Balázs
B
National Medical Center, Institute of Haematology and Immunology, Membrane Research Group of the Hungarian Academy of Sciences, Diószegi u. 64, H-1113 Budapest, Hungary. sarkadi@biomembrane.hu
Ozvegy-Laczka
Csilla
C
Német
Katalin
K
Váradi
András
A
D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000235:genetics / Q000378:metabolism / Q000502:physiology*; D000818:Animals; D001692:Biological Transport; D004351:Drug Resistance; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D015316:Genetic Therapy; D006801:Humans; D000860:Hypoxia; D008954:Models, Biological; D008957:Models, Genetic; D009363:Neoplasm Proteins / Q000235:genetics / Q000378:metabolism / Q000502:physiology*; D011110:Polymorphism, Genetic; D017434:Protein Structure, Tertiary; D013234:Stem Cells / Q000166:cytology; D014018:Tissue Distribution
C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D009363:Neoplasm Proteins