Interplay of breast cancer resistance protein (BCRP) and metabolizing enzy

Ye Tian, Yicong Bian, Yan Jiang, Sainan Qian, Aiming Yu, Su Zeng

Research output: Contribution to journalArticle

9 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)877-893
Number of pages17
JournalCurrent Drug Metabolism
Volume16
Issue number10
StatePublished - Dec 1 2015

Keywords

  • BCRP
  • Elimination
  • Interplay
  • Organs
  • Phase I metabolizing enzymes
  • Phase II metabolizing enzymes

ASJC Scopus subject areas

  • Pharmacology
  • Clinical Biochemistry

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  • Cite this

    Tian, Y., Bian, Y., Jiang, Y., Qian, S., Yu, A., & Zeng, S. (2015). Interplay of breast cancer resistance protein (BCRP) and metabolizing enzy. Current Drug Metabolism, 16(10), 877-893.