Journal
XENOBIOTICA
Volume 50, Issue 3, Pages 297-317Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/00498254.2019.1629043
Keywords
OATP; solute carrier; genetic polymorphism; hepatocyte; pharmacokinetics
Categories
Funding
- Priority Academic Program Development of the Jiangsu Higher Education Institutes (PAPD)
- Student's Platform for Innovation and Entrepreneurship Training Program of Soochow University [2018xj069]
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1. Organic anion transporting polypeptides (OATPs) belong to the superfamily of solute carriers (SLC), which are important membrane transporters in animals and humans. Liver is an important organ for drug disposition. In human liver, three OATPs, namely OATP1B1, 1B3 and 2B1, are expressed on the basolateral membrane of hepatocytes. 2. OATPs have multiple substrate specificity, mediating transport of a wide range of endo- and exogenous substances such as bile salts, bilirubin, hormones and their conjugates, toxins and various drugs. Therefore, they are important for drug disposition in human body. In this review, we compiled a complete list of the substrates for human hepatic OATPs. 3. OATP genes have single-nucleotide polymorphisms (SNPs), which could lead to the alteration of their function, and thus might result in the change of pharmacokinetic properties for their substrate drugs. In this review, we summarized the genetic polymorphisms of the three hepatic OATPs and their effect on in vitro transport function and in vivo pharmacokinetics of substrate drugs. 4. Finally, some concerns and perspectives on OATP polymorphism research are discussed.
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