2.A.60.1.12
OATP8/OATP1B3 (SLC21A8, SLCO1B3, OAT1B3, LST2, Ct-OAT1B3 isoform 1). The bile acid (cholic acid)/glutathione (GSH:bile acid = 2.1) exporter (Briz et al., 2006). Also transports the octapeptide, cholecystokinin (CCK-8) (Gui and Hagenbuch, 2008), the anticancer agent, methotrexate, the statin, rosuvastatin (Nigam 2015), and danoprevir (hepatitis C virus protease inhibitor) (Brennan et al. 2015). Forms homo and hetero oligomers, but the monomer is the active species (Zhang et al. 2017). It has been used as a dual reporter gene for fluorescence and magnetic resonance imaging (Wu et al. 2018).  It mediates the Na⁺-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). It is involved in the clearance of bile acids and organic anions from the liver (van de Steeg et al. 2012). Gly45 and Phe555 in TMSs 1 and 10 are critical for activation by epigallocatechin gallate (Yue et al. 2019). Rare coding variants that cause changes of charged residues can have large effects on the function and expression of OAT1B3 (Liu et al. 2021). Val386 in TMS 8 is important for the activation of OATP1B3 by epigallocatechin gallate (Wang et al. 2022). Cancer-type organic anion-transporting polypeptide 1B3 (Ct-OATP1B3) is localized to lysosomes and mediates resistance against kinase inhibitors (Brennan et al. 2015). Forms homo and hetero oligomers, but the monomer is the active species (Zhang et al. 2017). It has been used as a dual reporter gene for fluorescence and magnetic resonance imaging (Wu et al. 2018).  It mediates the Na⁺-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). It is involved in the clearance of bile acids and organic anions from the liver (van de Steeg et al. 2012). Gly45 and Phe555 in TMSs 1 and 10 are critical for activation by epigallocatechin gallate (Yue et al. 2019). Rare coding variants that cause changes of charged residues can have large effects on the function and expression of OAT1B3 (Liu et al. 2021). Val386 in TMS 8 is important for the activation of OATP1B3 by epigallocatechin gallate (Wang et al. 2022). Cancer-type organic anion-transporting polypeptide 1B3 (Ct-OATP1B3) is localized to lysosomes and mediates resistance against kinase inhibitors (Haberkorn et al. 2022).