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OATP2A1 (SLCO2A1)

Molecular structure and tissue distribution
The human organic anion-transporting polypeptide 2A1 (OATP2A1) is a prostaglandin transporter expressed in several tissues and plays an important role for local distribution of prostaglandins. Significant protein expression of human OATP2A1 were demonstrated in retinal epithelial cells, in epithelial and endothelial cell layers different eye tissues, parietal cells of the gastric corpus and pyloric gland of antrum, in kidney proximal tubule, neurons, astrocytes and microglia. Human OATP2A1 protein consists of 643 amino acids. Overall, the humane OATPs possess 60% amino acid sequence identity.


Interaction of hOATP2A1 with endogenous compounds and drugs

Human OATP2A1 transports various prostaglandins including PGE1, PGE2, PGD2, and PGF2. OATP2A1 mediates the release of newly synthesized prostaglandins from cells, the transepithelial transport of prostaglandins, and the clearance of prostaglandins from the circulation.
Physiologically OATP2A1 plays an important role in the stomach. This transporter is involved in the uptake of prostaglandin in gastric epithelial cells and terminates the regulatory effect of PGE2 on the acid (HCl) secretin. A commonly used reference substrate for OATP2A1 is prostaglandin-E2.The PGE2 uptake is significantly reduced by cyclooxygenase inhibitors diclofenac and lumiracoxib in contrast salicylic acid, indomethacin, ibuprofen and ketoprofen stimulate the OATP2A1 facilitated PGE2 transport.
Latanoprost is a drug used in the local treatment of glaucoma as well as elevated intraocular pressure. For this purpose it is applied in the form of eye drops. The latanoprost acid uptake in eye is mediated effectively by OATP2A1.

Figure 1Time dependent uptake of PGE2 in hOATP2A1 and vector transfected HEK293 cells Figure 2 Concentration dependent uptake of PGE2 in hOATP2A1 transfected HEK293 cells
 

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