title: Interplay of Breast Cancer Resistance Protein (BCRP) and Metabolizing Enzymes.
abstract: The recent identification of the interplay between metabolizing enzymes and BCRP has drawn more and more attention from people. BCRP, a transporter belonging to ATP-binding cassette (ABC) family, has been hypothesized to play roles in many aspects including protecting the human body against therapeutics because it is expressed in the tissues that function as barriers in vivo. Efficient coupling of BCRP and metabolizing enzymes enables rapid elimination of foreign compounds from the body because BCRP could facilitate the excretion of metabolites catalyzed by phase I and II enzymes into bile, urine and feces. Without BCRP coupling, pass through the cell membrane may be difficult for them by passive diffusion because of the increment of the molecular weight and water solubility. Thus the metabolism-efflux alliance has extraordinary importance to drug metabolism, distribution, pharmacological effect, toxicity and elimination. In this manuscript, a brief discussion about the interplays of BCRP and metabolizing enzymes in liver, intestine, kidney, lung and other organs were presented and summarized. Many endogenous and exogenous compounds belong to different chemical groups, for instance, the dietary flavonoids and the steroidal hormones were involved. Clarifying the cooperation mechanisms of BCRP and enzymes could lead to a better prediction of drug clearance in vitro.
authors.forename: Ye
authors.initials: Y
authors.lastname: Tian
authors.forename: Yicong
authors.initials: Y
authors.lastname: Bian
authors.forename: Yan
authors.initials: Y
authors.lastname: Jiang
authors.forename: Sainan
authors.initials: S
authors.lastname: Qian
authors.forename: Aiming
authors.initials: A
authors.lastname: Yu
authors.affiliation: College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, Zhejiang Province, P. R. China. zengsu@zju.edu.cn.
authors.forename: Su
authors.initials: S
authors.lastname: Zeng
mesh_terms: D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000378:metabolism*; D000818:Animals; D002462:Cell Membrane / Q000378:metabolism; D004798:Enzymes / Q000378:metabolism*; D006801:Humans; D008970:Molecular Weight; D009363:Neoplasm Proteins / Q000378:metabolism*; D004364:Pharmaceutical Preparations / Q000737:chemistry / Q000378:metabolism*; D012995:Solubility; D015262:Xenobiotics / Q000737:chemistry / Q000378:metabolism
chemical_list: C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D004798:Enzymes; D009363:Neoplasm Proteins; D004364:Pharmaceutical Preparations; D015262:Xenobiotics