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ABCG2 – a transporter for all seasons
Author(s) -
Sarkadi Balázs,
Özvegy-Laczka Csilla,
Német Katalin,
Váradi András
Publication year - 2004
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2004.03.123
Subject(s) - abcg2 , transporter , stem cell , efflux , biology , atp binding cassette transporter , microbiology and biotechnology , p glycoprotein , pharmacology , gene , multiple drug resistance , biochemistry , drug resistance , genetics
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.