Organic Anion Transporting Polypeptide Family

Organic Anion Transporting Polypeptide Family (OATP)... 

Schiffer, R., Neis, M., Holler, D., et al. Active influx transport is mediated by members of the organic anion transporting polypeptide family in human epidermal ker-atinocytes. J. Invest. Dermatol. 120(2) 285-291, 2003. 

Shimizu, M., Fuse, K., Okudaira, K., Nishigaki, R., Maeda, K., Kusuhara, H. and Sugiyama, Y. (2005) Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Drug Metabolism and Disposition The Biological Fate of Chemicals, 33, 1477-1481. 

The organic anion transporting polypeptides (rodents Oatps human OATPs) represent a family of proteins responsible for the membrane transport of a large number of endogenous and xenobiotic compounds with diverse chemical characteristics. Since the first expression of Oatplal in 1994, organic anion transporting polypeptide family members have been isolated from a variety of tissues in vertebrate animal species [1]. 

Organic anion transporters can be divided into three major families organic anion transporters (OATs), organic anion transporting polypeptides (OATPs), and multidrug resistance associated proteins (MRPs) [201]. 

Hagenbuch, B. and Meier, P.J. (2004) Organic anion transporting polypeptides ofthe OATP/SLC21 family phylogenetic classification as OATP/SLCO superfamily, new nomenclature and molecular/functional properties. 

Other mechanisms of interaction have also been reported, such as altered activity of other enzymes within the CYP450 family (14—17). Moreover, GFJ may also inhibit the intestinal P-glycoprotein (P-gp)-mediated efflux transport of drugs such as cyclosporine to increase its oral bioavailability (18-21). GFJ and other fruit juices have recently been shown to be potent in vitro inhibitors of a number of organic anion-transporting polypeptides (OATPs) (22,23). 

Kim RB. Organic anion-transporting polypeptide (OATP) transporter family and drug disposition. Eur J Clin Invest 2003 33(suppl 2) 1-5. 

Organic Anion Transporting Polypeptide (OATP/SLCO) Family... 

D-Ala-deltorphin-I and -II transverse the blood brain barrier in vivo and in vitro [51]. Recently, D-Ala-deltorphin-II was identified as a transport substrate of organic anion transporting polypeptides (Oatp/OATP), a family of polyspecific membrane transporters, strongly expressed at the rat and human blood brain barrier [52]. Modified analogues of these peptides were synthesized to improve their transit across the blood brain barrier [48,49,53]. Because they resist enzyme degradation and can cross endothelial barriers into the CNS, the deltorphins meet the criteria for peptides with potential for systemic administration. 

Kobayashi D, Nozawa T, Imai K et al. (2003) Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH dependent transport across intestinal apical membrane. J Pharmacol Exp Therap 306 703-708 Koepsell H, Endou H (2004) The SLC22 drug transporter family. Pflugers Arch 447(5) 666-676... 

Table 5. Organic anion transporter (OAT) and organic anion transporting polypeptide (OATP) families (from [34], with permission).

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