General Information of the Protein
Protein ID
PT05092
Protein Name
Organic anion transporter 3
Secondarily
Protein Name
Organic anion/dicarboxylate exchanger
Solute carrier family 22 member 8
Gene Name
SLC22A8
Secondarily
Gene Name
Oat3
Sequence
MTFSEILDRVGSMGPFQYLHVTLLALPVLGIANHNLLQIFTATTPVHHCRPPPNASIGPWVLPLDPNGKPEKCLRFVHLPNASLPNDTQRATEPCLDGWIYNSTRDTIVIEWDLVCSSNKLKEMAQSIFMAGILVGGPVIGELSDRFGRKPILTWSYLMLAASGSGAAFSPSLPVYMIFRFLCGCSISGISLSTVILNVEWVPTSMRAISSTSIGYCYTIGQFILSGLAYAIPQWRWLQLTSSAPFFIFSLLSWWVPESIRWLVLSGKYSKALKTLQRVATFNGKKEEGKKLTIEELKFNLQKDITSAKVKYGLSDLFRVSILRRVTFCLSLAWFSTGFAYYSLAMGVEEFGVNIYILQIIFGGVDIPAKFITILSLSYLGRRITQSFLLLLAGGAILALIFVPSEMQLLRTALAVFGKGCLSGSFSCLFLYTSELYPTVLRQTGMGISNVWARVGSMIAPLVKITGELQPFIPNVIFGTTALLGGSAAFFLLETLNRPLPETIEDIQNWHKQVQKTKQESEAEKASQIIPLKTGG
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Organism
Rattus norvegicus, Rat
Protein Classification
Transporter
>
Electrochemical transporter
>
SLC superfamily of solute carriers
>
SLC22 family of organic cation and anion transporters
Function
Functions as an organic anion/dicarboxylate exchanger that couples organic anion uptake indirectly to the sodium gradient (PubMed:12660303, PubMed:12488248). Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) (PubMed:12660303, PubMed:12488248, PubMed:23832370). Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain (PubMed:10224140, PubMed:11961115, PubMed:12684544). E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange (By similarity). Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule (By similarity). Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate (PubMed:23832370). Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins (By similarity). May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside (By similarity). May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate (By similarity). Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) (PubMed:11861777, PubMed:12660303, PubMed:14675047, PubMed:15846470). May contribute to the release of cortisol in the adrenals (By similarity). Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (PubMed:11961115, PubMed:15319347, PubMed:15389674). Regulates the CSF concentration of histamine H(2)-receptor antagonists cimetidine and ranitidine at the CP (PubMed:15319347). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the uptake from brain of organic anions, such as E1S, PAH, and OTA (PubMed:10224140, PubMed:11961115). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB) (PubMed:11961115, PubMed:12684544, PubMed:15292460). In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (PubMed:15292460).
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Uniprot ID
Primary ID:
Q9R1U7

Secondarily ID:
Q66HN0
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Ensembl ID
ENSG00000149452
Subcellular Location
Basolateral cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000009 , LLC-PK1
Compound ID Compound Name Compound Formula
CP0069674
4-Dipropylsulfamoyl-benzoic acid
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C13H19NO4S
 2
1
Ki = 4430 nM
   TI
   LI
   LO
   TS
2
Ki = 20000 nM
   TI
   LI
   LO
   TS
CP0127632
ESTRONE
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C18H22O5S
 1
1
Ki = 9100 nM
   TI
   LI
   LO
   TS
CP0256501
17beta-Estradiol-17-(beta-D-glucuronide)
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C24H32O8
 1
1
Ki = 35600 nM
   TI
   LI
   LO
   TS
CP0035927
(Cimetidine) N-Methyl-N''''-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine,cyanide
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C10H16N6S
 1
1
Ki = 46800 nM
   TI
   LI
   LO
   TS
CP0034782
(+)-3,3-Dimethyl-7-oxo-6-phenylacetylamino-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylic acid(penicillin G)
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C16H18N2O4S
 1
1
Km = 82600 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02209 Organic anion transporter 3 Homo sapiens, Human
PT06258 Organic anion transporter 3 Mus musculus, Mouse