Polymorphisms of the Multidrug Pump ABCG2: A Systematic Review of Their Effect on Protein Expression, Function, and Drug Pharmacokinetics

• Published in: Drug metabolism and disposition Vol. 46; no. 12; pp. 1886 - 1899
• Main Authors: Heyes, Niall, Kapoor, Parth, Kerr, Ian D.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.12.2018; American Society for Pharmacology and Experimental Therapeutics, Inc
• Subjects: Anticancer properties; Antitumor agents; ATP Binding Cassette Transporter, Subfamily G, Member 2 - genetics; ATP Binding Cassette Transporter, Subfamily G, Member 2 - physiology; Blood groups; Cancer; Drug Resistance, Multiple; Efflux; Humans; Inspection; Mitoxantrone; Pharmaceutical Preparations - metabolism; Pharmacokinetics; Pharmacology; Polymorphism; Polymorphism, Single Nucleotide; Protein-tyrosine kinase; Proteins; Single-nucleotide polymorphism; Substrates; Tyrosine; NBD; ABC; TKI; SNP; Jr; TM; MDR; SASP; WT; AUC; MSD

The widespread expression and polyspecificity of the multidrug ABCG2 efflux transporter make it an important determinant of the pharmacokinetics of a variety of substrate drugs. Null ABCG2 expression has been linked to the Junior blood group. Polymorphisms affecting the expression or function of ABC...