Interrelationship Between Substrates and Inhibitors of Human CYP3A and P-Glycoprotein

被引:0
|
作者
Richard B. Kirn
Christoph Wandel
Brenda Leake
Mirjana Cvetkovic
Martin F. Fromm
Peter J. Dempsey
Mark M. Roden
Frank Belas
Ajai K. Chaudhary
Dan M. Roden
Alastair J. J. Wood
Grant R. Wilkinson
机构
[1] Vanderbilt University School of Medicine,Departments of Medicine and Pharmacology
关键词
CYP3A4; P-glycoprotein; drug transport; cytochrome P450;
D O I
10.1023/A:1018877803319
中图分类号
学科分类号
摘要
Purpose. CYP3A and P-gp both function to reduce the intracellular concentration of drug substrates, one by metabolism and the other by transmembrane efflux. Moreover, it has been serendipitously noted that the two proteins have many common substrates and inhibitors. In order to test this notion more fully, systematic studies were undertaken to determine the P-gp-mediated transport and inhibitory characteristics of prototypical CYP substrates.
引用
收藏
页码:408 / 414
页数:6
相关论文
共 50 条
  • [31] Do men and women differ in proximal small intestinal CYP3A or P-glycoprotein expression?
    Paine, MF
    Ludington, SS
    Chen, ML
    Stewart, PW
    Huang, SM
    Watkins, PB
    DRUG METABOLISM AND DISPOSITION, 2005, 33 (03) : 426 - 433
  • [33] P-glycoprotein deficiency enhances metabolic activation of and platelet response to clopidogrel through marked up-regulation of Cyp3a11 in mice: Direct evidence for the interplay between P-glycoprotein and Cyp3a
    Ji, Jin-Zi
    Li, Yi-Fei
    Jiang, Li-Ping
    Tai, Ting
    Ge, Peng-Xin
    Mi, Qiong-Yu
    Zhu, Ting
    Xie, Hong-Guang
    BIOCHEMICAL PHARMACOLOGY, 2021, 183
  • [34] Ontogeny of CYP3A and P-Glycoprotein in the Liver and the Small Intestine of the Gottingen Minipig: An Immunohistochemical Evaluation
    Van Peer, Els
    Verbueken, Evy
    Saad, Moayad
    Casteleyn, Christophe
    Van Ginneken, Chris
    Van Cruchten, Steven
    BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY, 2014, 114 (05) : 387 - 394
  • [35] The impact of P-glycoprotein, breast cancer resistance protein and CYP3A on pharmacokinetics and metabolism of galunisertib
    Li, Wenlong
    Tibben, Matthijs
    Wang, Yaogeng
    Lebre, Maria C.
    Rosing, Hilde
    Beijnen, Jos H.
    Schinkel, Alfred H.
    CANCER RESEARCH, 2019, 79 (13)
  • [36] Fexofenadine and midazolam disposition in relation to genetic polymorphisms of CYP3A, PXR and P-glycoprotein (PGP)
    Xie, R
    Knuth, DM
    Tan, L
    Polasek, EC
    Hong, C
    Teillol-Foo, M
    Antal, EJ
    CLINICAL PHARMACOLOGY & THERAPEUTICS, 2003, 73 (02) : P19 - P19
  • [37] Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A
    Bekaii-Saab, TS
    Perloff, MD
    Weemhoff, JL
    Greenblatt, DJ
    von Moltke, LL
    BIOPHARMACEUTICS & DRUG DISPOSITION, 2004, 25 (07) : 283 - 289
  • [38] Characterisation of β-adrenoreceptor antagonists as substrates and inhibitors of P-glycoprotein
    Bachmakov, I
    Werner, U
    Endress, B
    Auge, D
    Fromm, MF
    EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, 2005, 61 (09) : 702 - 702
  • [39] Computational models for predicting substrates or inhibitors of P-glycoprotein
    Chen, Lei
    Li, Youyong
    Zhang, Huidong
    Zhang, Liling
    Hou, Tingjun
    DRUG DISCOVERY TODAY, 2012, 17 (7-8) : 343 - 351
  • [40] Quantitative evaluation of isothiocyanates as substrates and inhibitors of P-glycoprotein
    Barecki-Roach, M
    Wang, EJ
    Johnson, WW
    JOURNAL OF PHARMACY AND PHARMACOLOGY, 2003, 55 (09) : 1251 - 1257