Title:Interplay of Breast Cancer Resistance Protein (BCRP) and Metabolizing Enzymes
Volume: 16
Issue: 10
Author(s): Ye Tian, Yicong Bian, Yan Jiang, Sainan Qian, Aiming Yu and Su Zeng
Affiliation:
Keywords:
BCRP, elimination, interplay, organs, phase I metabolizing enzymes, phase II 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.