Journal
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 52
Volume 52, Issue -, Pages 135-151Publisher
ANNUAL REVIEWS
DOI: 10.1146/annurev-pharmtox-010510-100556
Keywords
uptake transporter; cancer therapeutics; anticancer drugs; OATP
Categories
Funding
- NATIONAL CENTER FOR RESEARCH RESOURCES [P20RR021940] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM077336] Funding Source: NIH RePORTER
- NCRR NIH HHS [P20 RR021940, P20 RR021940-05] Funding Source: Medline
- NIGMS NIH HHS [R01 GM077336-04, R01 GM077336] Funding Source: Medline
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Organic anion transporting polypeptides (OATPs) are members of the SLCO gene superfamily of proteins. The 11 human OATPs are classified into 6 families and subfamilies on the basis of their amino acid sequence similarities. OATPs are expressed in several epithelial tissues throughout the body and transport mainly amphipathic molecules with molecular weights of more than 300 kDa. Members of the OATP1 and OATP2 families are functionally the best-characterized OATPs. Among these are the multispecific OATP1A2, OATP1B1, OATP1B3, and OATP2B1. They transport various endo- and xenobiotics, including hormones and their conjugates as well as numerous drugs such as several anticancer agents. Recent reports demonstrate that some OATPs are up- or downregulated in several cancers and that OATP expression might affect cancer development. On the basis of the findings summarized in this review, we propose that OATPs could be valuable targets for anticancer therapy.
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