Int J Biochem Mol Biol 2012;3(1):1-27
Review Article
Human ABCG2: structure, function, and its role in multidrug resistance
Wei Mo, Jian-Ting Zhang
Department of Pharmacology and Toxicology and IU Simon Cancer Center, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
Received March 16, 2012; accepted March 25, 2011; Epub March 30, 2011; Published March 30, 2012
Abstract: Human ABCG2 is a member of the ATP-binding cassette (ABC) transporter superfamily and is known to contribute to multidrug
resistance (MDR) in cancer chemotherapy. Among ABC transporters that are known to cause MDR, ABCG2 is particularly interesting for its
potential role in protecting cancer stem cells and its complex oligomeric structure. Recent studies have also revealed that the biogenesis of
ABCG2 could be modulated by small molecule compounds. These modulators, upon binding to ABCG2, accelerate the endocytosis and
trafficking to lysosome for degradation and effectively reduce the half-life of ABCG2. Hence, targeting ABCG2 stability could be a new venue for
therapeutic discovery to sensitize drug resistance human cancers. In this report, we review recent progress on understanding the structure,
function, biogenesis, as well as physiological and pathophysiological functions of ABCG2. (IJBMB1201005).
Keywords: Human ABCG2, structure, function, multidrug resistance, ATP-binding cassette, cancer, chemotherapy
Address all correspondence to:
Dr. Jian-Ting Zhang
IU Simon Cancer Center
980 W. Walnut St., R3-C510
Indianapolis, IN 46202, USA.
Tel: (317) 278-4503; Fax: (317) 274-8046
E-mail jianzhan@iupui.edu
Review Article
Human ABCG2: structure, function, and its role in multidrug resistance
Wei Mo, Jian-Ting Zhang
Department of Pharmacology and Toxicology and IU Simon Cancer Center, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
Received March 16, 2012; accepted March 25, 2011; Epub March 30, 2011; Published March 30, 2012
Abstract: Human ABCG2 is a member of the ATP-binding cassette (ABC) transporter superfamily and is known to contribute to multidrug
resistance (MDR) in cancer chemotherapy. Among ABC transporters that are known to cause MDR, ABCG2 is particularly interesting for its
potential role in protecting cancer stem cells and its complex oligomeric structure. Recent studies have also revealed that the biogenesis of
ABCG2 could be modulated by small molecule compounds. These modulators, upon binding to ABCG2, accelerate the endocytosis and
trafficking to lysosome for degradation and effectively reduce the half-life of ABCG2. Hence, targeting ABCG2 stability could be a new venue for
therapeutic discovery to sensitize drug resistance human cancers. In this report, we review recent progress on understanding the structure,
function, biogenesis, as well as physiological and pathophysiological functions of ABCG2. (IJBMB1201005).
Keywords: Human ABCG2, structure, function, multidrug resistance, ATP-binding cassette, cancer, chemotherapy
Address all correspondence to:
Dr. Jian-Ting Zhang
IU Simon Cancer Center
980 W. Walnut St., R3-C510
Indianapolis, IN 46202, USA.
Tel: (317) 278-4503; Fax: (317) 274-8046
E-mail jianzhan@iupui.edu
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