title: Organic anion-transporting polypeptides: a novel approach for cancer therapy.
abstract: Organic anion-transporting polypeptides (OATPs) encoded by the SLCO genes constitute an important transporter superfamily that mediates transmembrane transport of various clinical drugs and endogenous nutrients. Eleven human OATPs with different transport functions are expressed in various tissues. Bile acids, steroid hormone conjugates, prostaglandins, testosterone and thyroid hormones that promote cell proliferation are typical substrates of OATPs. Many important clinical drugs have been identified as substrates of OATP1B1, OATP1B3, OATP2B1 and OATP1A2. Liver-specific OATP1B1 and OATP1B3 as well as testis-specific OATP6A1 are expressed in malignancies and can act as biomarkers for many tumours. Various studies have shown the associations of genetic polymorphisms in OATP genes with the uptake pharmacokinetics of their substrates. Because of their abundant expression in tumours and their high transport activity for many cancer drugs, OATPs should be considered as important therapeutic targets in anti-cancer drug design.
authors.affiliation: State Engineering Laboratory of Bio-Resources Eco-Utilization, Northeast Forestry University, Ministry of Education , Harbin , China and.
authors.forename: Tianyu
authors.initials: T
authors.lastname: Liu
authors.forename: Qingyong
authors.initials: Q
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use*; D014408:Biomarkers, Tumor / Q000378:metabolism; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism*; D027361:Organic Anion Transporters / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D014408:Biomarkers, Tumor; D027361:Organic Anion Transporters