General Information of Target

Target ID LDTP09945
Target Name Solute carrier organic anion transporter family member 2A1 (SLCO2A1)
Gene Name SLCO2A1
Gene ID 6578
Synonyms
OATP2A1; SLC21A2; Solute carrier organic anion transporter family member 2A1; SLCO2A1; OATP2A1; PHOAR2; Prostaglandin transporter; PGT; Solute carrier family 21 member 2; SLC21A2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEPPGDWGPPPWRSTPKTDVLRLVLYLTFLGAPCYAPALPSCKEDEYPVGSECCPKCSPG
YRVKEACGELTGTVCEPCPPGTYIAHLNGLSKCLQCQMCDPAMGLRASRNCSRTENAVCG
CSPGHFCIVQDGDHCAACRAYATSSPGQRVQKGGTESQDTLCQNCPPGTFSPNGTLEECQ
HQTKCSWLVTKAGAGTSSSHWVWWFLSGSLVIVIVCSTVGLIICVKRRKPRGDVVKVIVS
VQRKRQEAEGEATVIEALQAPPDVTTVAVEETIPSFTGRSPNH
Target Type
Patented-recorded
Target Bioclass
Transporter and channel
Family
Organo anion transporter (TC 2.A.60) family
Subcellular location
Cell membrane
Function
Mediates the transport of prostaglandins (PGs, mainly PGE2, PGE1, PGE3, PGF2alpha, PGD2, PGH2) and thromboxanes (thromboxane B2) across the cell membrane. PGs and thromboxanes play fundamental roles in diverse functions such as intraocular pressure, gastric acid secretion, renal salt and water transport, vascular tone, and fever. Plays a role in the clearance of PGs from the circulation through cellular uptake, which allows cytoplasmic oxidation and PG signal termination. PG uptake is dependent upon membrane potential and involves exchange of a monovalent anionic substrate (PGs exist physiologically as an anionic monovalent form) with a stoichiometry of 1:1 for divalent anions or of 1:2 for monovalent anions. Uses lactate, generated by glycolysis, as a counter-substrate to mediate PGE2 influx and efflux. Under nonglycolytic conditions, metabolites other than lactate might serve as counter-substrates. Although the mechanism is not clear, this transporter can function in bidirectional mode. When apically expressed in epithelial cells, it facilitates transcellular transport (also called vectorial release), extracting PG from the apical medium and facilitating transport across the cell toward the basolateral side, whereupon the PG exits the cell by simple diffusion. In the renal collecting duct, regulates renal Na+ balance by removing PGE2 from apical medium (PGE2 EP4 receptor is likely localized to the luminal/apical membrane and stimulates Na+ resorption) and transporting it toward the basolateral membrane (where PGE2 EP1 and EP3 receptors inhibit Na+ resorption). Plays a role in endometrium during decidualization, increasing uptake of PGs by decidual cells. Involved in critical events for ovulation. Regulates extracellular PGE2 concentration for follicular development in the ovaries. Expressed intracellularly, may contribute to vesicular uptake of newly synthesized intracellular PGs, thereby facilitating exocytotic secretion of PGs without being metabolized. Essential core component of the major type of large-conductance anion channel, Maxi-Cl, which plays essential roles in inorganic anion transport, cell volume regulation and release of ATP and glutamate not only in physiological processes but also in pathological processes. May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable).
TTD ID
T15518
Uniprot ID
Q92959
DrugMap ID
TTKVTQO
Ensemble ID
ENST00000310926.11
HGNC ID
HGNC:10955
ChEMBL ID
CHEMBL2073703

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C594(1.10)  LDD0078  [1]
Acrolein
 Probe Info 
N.A.  LDD0217  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0020  ARS-1620 HCC44 C594(1.10)  LDD0078  [1]
 LDCM0022  KB02 G361 C587(2.32)  LDD2477  [3]
 LDCM0023  KB03 CHL1 C587(1.61)  LDD2892  [3]
 LDCM0024  KB05 G361 C587(2.82)  LDD3311  [3]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alprostadil Small molecular drug DB00770
Dinoprost Tromethamine Small molecular drug DB01160
Dinoprostone Small molecular drug DB00917
Furosemide Small molecular drug DB00695
Iloprost Small molecular drug DB01088
Lactic Acid Small molecular drug DB04398
Latanoprost Small molecular drug DB00654
Phenobarbital Small molecular drug DB01174
Pyruvic Acid Small molecular drug DB00119
Rifamycin Small molecular drug DB11753
Investigative
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Arachidonic Acid Small molecular drug DB04557
Bromocresol Green Small molecular drug D0KO9R
Bromsulphthalein Small molecular drug D0W8GY
Glucose-6-phosphate Small molecular drug DB03581
Phosphoenolpyruvate Small molecular drug DB01819
Prostaglandin D2 Small molecular drug DB02056
Beta-d-fructofuranose 16-bisphosphate . DB04551
D-glyceraldehyde 3-phosphate . DB02263
Patented
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid26099857-compound-wo2011037610formula(I) Small molecular drug D07XPI

References

1 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
2 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
3 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840