SLCO1A2
Domain
A conserved histidine residue in the third TMD (His-107) may play an essential role in the pH sensitivity of SLCO1A2/OATP1A2-mediated substrate transport.
Function
Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane (PubMed:19129463, PubMed:7557095). Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) (PubMed:11159893, PubMed:12568656, PubMed:19129463, PubMed:23918469, PubMed:25560245, PubMed:9539145). Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision (PubMed:25560245). Involved in the uptake of clinically used drugs (PubMed:17301733, PubMed:20686826, PubMed:27777271). Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) (PubMed:19129463, PubMed:20358049). Also transports prostaglandin E2 (PubMed:19129463). Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons (PubMed:25132355). May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel (PubMed:23243220). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment (PubMed:19129463). Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions (PubMed:19129463). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable).
Sequence Similarities
Belongs to the organo anion transporter (TC 2.A.60) family.
Tissue Specificity
Higher expression in the brain than in liver and kidney (PubMed:15632119, PubMed:7557095, PubMed:9539145). Expressed in brain neurons in both cortex and hippocampus (PubMed:10873595, PubMed:25132355). Expressed in placental trophoblasts (PubMed:12409283). Also expressed in lung and testes at lower levels (PubMed:7557095). Expressed in the eye (at protein level) (PubMed:25560245). Expressed in the retina in the outer and inner nuclear layers, the inner plexiform layer and the ganglion cell layer (PubMed:25132355). Expressed in liver and prostate (PubMed:10873595). In testis, primarily localized to the basal membrane of Sertoli cells and weakly expressed in Leydig cells and within the tubules (PubMed:35307651). Expressed in fetal brain and liver (PubMed:10873595).
Cellular localization
- Cell membrane
- Multi-pass membrane protein
- Basal cell membrane
- Multi-pass membrane protein
- Localized to the basal membrane of Sertoli cells.
Alternative names
OATP, OATP1, OATP1A2, SLC21A3, SLCO1A2, Solute carrier organic anion transporter family member 1A2, OATP-A, Organic anion-transporting polypeptide 1, Sodium-independent organic anion transporter, Solute carrier family 21 member 3, OATP-1