ATP-binding cassette super-family G member 2 is a protein that in humans is encoded by the ABCG2 gene.[6][7] ABCG2 has also been designated as CDw338 (cluster of differentiation w338). ABCG2 is a translocation protein used to actively pump drugs and other compounds against their concentration gradient using the bonding and hydrolysis of ATP as the energy source.[1]
ABCG2 forms into a homodimer to assume its active transport conformation. The dimer weighs approximately 144 kDa. The expression of this transport protein is highly conserved throughout the animal kingdom, pointing to its importance.[8]
Substrate binding with compounds occurs in the large central cavity. ABCG2 can bind to a broad range of compounds but binds strongest to flat, polycyclic chemicals with lots of hydrophobic character.[1]
^ abcTaylor NM, Manolaridis I, Jackson SM, Kowal J, Stahlberg H, Locher KP (June 2017). "Structure of the human multidrug transporter ABCG2". Nature. 546 (7659): 504–509. Bibcode:2017Natur.546..504T. doi:10.1038/nature22345. hdl:20.500.11850/233014. PMID 28554189. S2CID 4461745.
^ abcGRCh38: Ensembl release 89: ENSG00000118777 – Ensembl, May 2017
^ abcGRCm38: Ensembl release 89: ENSMUSG00000029802 – Ensembl, May 2017
^"Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^"Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^Allikmets R, Gerrard B, Hutchinson A, Dean M (October 1996). "Characterization of the human ABC superfamily: isolation and mapping of 21 new genes using the expressed sequence tags database". Human Molecular Genetics. 5 (10): 1649–1655. doi:10.1093/hmg/5.10.1649. PMID 8894702.
^Doyle LA, Yang W, Abruzzo LV, Krogmann T, Gao Y, Rishi AK, Ross DD (December 1998). "A multidrug resistance transporter from human MCF-7 breast cancer cells". Proceedings of the National Academy of Sciences of the United States of America. 95 (26): 15665–15670. Bibcode:1998PNAS...9515665D. doi:10.1073/pnas.95.26.15665. PMC 28101. PMID 9861027.
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in humans is encoded by the ABCG2 gene. ABCG2 has also been designated as CDw338 (cluster of differentiation w338). ABCG2 is a translocation protein used...
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from decreased deoxycytidine kinase activity in vitro. ABC transporter ABCG2 promotes export of clofarabine-5´-monophosphate and thus limits the cytotoxic...
antineoplastic drugs. The study showed that apatinib reverses the ABCB1- and ABCG2-mediated multidrug resistance by inhibiting those functions and increasing...
inhibitor and a substrate of the transporter proteins P-glycoprotein (Pgp), ABCG2, OATP1B1 and OATP1B3. It is partly degraded by the liver enzymes CYP2B6...
"Avapritinib: A Selective Inhibitor of KIT and PDGFRα that Reverses ABCB1 and ABCG2-Mediated Multidrug Resistance in Cancer Cell Lines". Mol. Pharm. 16 (7):...
proteins ABCG2 (breast cancer resistance protein, BCRP) and P-glycoprotein (P-gp), which has been shown to increase plasma concentrations of the ABCG2 substrate...
Sissung TM, Burger H, Nooter K, Soepenberg O, et al. (July 2004). "Effect of ABCG2 genotype and mRNA expression on the bioavailability of topotecan". Journal...
and weight standards Asset-backed commercial paper An alternate name for ABCG2, the human gene ATP-binding cassette, sub-family G (WHITE), member 2 As...
PMID 21295271. Scharenberg CW, Harkey MA, Torok-Storb B (January 2002). "The ABCG2 transporter is an efficient Hoechst 33342 efflux pump and is preferentially...
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