2.A.60.1.1 Organic anion transporter, Oatp1 (SLC21A1) (substrates: digoxin, bromosulfophthalein, conjugated (taurocholate) and unconjugated (cholate) bile salts; conjugated and unconjugated steroid hormones, eicosanoids, peptides, drugs, toxins, other organic anions (e.g., bilirubin, glucuronide) and organic cations (e.g., N-methylquinidine, rocuronium)) (Na+-independent). OATP models share a conserved transmembrane helix folding harbouring a
druggable binding pocket in the shape of an inner pore (Tonduru et al. 2022). Simulations
suggest that the conserved salt bridges in the extracellular region
between residues in TMS1 and TMS7 might influence the entrance of
substrates. Interactions between residues in TMS1 and TMS4 within OATP1
family members have shown their importance in transport of substrates (Tonduru et al. 2022).
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Accession Number: | P46720 |
Protein Name: | OATP1 aka Slc21a1 aka SLC21A3 |
Length: | 670 |
Molecular Weight: | 74178.00 |
Species: | Rattus norvegicus (Rat) [10116] |
Number of TMSs: | 12 |
Location1 / Topology2 / Orientation3: |
Membrane1 / Multi-pass membrane protein2 |
Substrate |
cholate, peptide, taurocholic acid, beta-D-glucosiduronic acid, bilirubin, icosanoid, steroid hormone, rocuronium bromide, bromosulfophthalein sodium, drug, toxin, digoxin |
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RefSeq: |
NP_058807.1
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Entrez Gene ID: |
50572
|
Pfam: |
PF07648
PF03137
|
KEGG: |
rno:50572
|
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[1] “Expression cloning of a rat liver Na(+)-independent organic anion transporter.” Jacquemin E. et.al. 8278353
[2] “Interaction with PDZK1 is required for expression of organic anion transporting protein 1A1 on the hepatocyte surface.” Wang P. et.al. 15994332
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1: MEETEKKIAT QEGRLFSKMK VFLLSLTCAC LTKSLSGVYM NSMLTQIERQ FDISTSVAGL
61: INGSFEIGNL FFIVFVSYFG TKLHRPVVIG IGCVIMGLGC LLMSLPHFFM GRYEYETTIS
121: PTGNLSSNSF LCMENRTQTL KPTQDPAECV KEMKSLMWIC VMVGNIIRGI GETPIVPLGI
181: SYIEDFAKSE NSPLYIGILE MGKVAGPIFG LLLGSYCAQI YVDIGSVNTD DLTITPSDTR
241: WVGAWWIGFL VCAGVNILTS IPFFFLPKAL PKKGQQENVA VTKDGKVEKY GGQAREENLG
301: ITKDFLTFMK RLFCNPIYML FILTSVLQVN GFINKFTFLP KYLEQQYGKS TAEAIFLIGV
361: YSLPPICLGY LIGGFIMKKF KITVKKAAYL AFCLSVFEYL LFLCHFMLTC DNAAVAGLTT
421: SYKGVQHQLH VESKVLADCN TRCSCSTNTW DPVCGDNGVA YMSACLAGCK KFVGTGTNMV
481: FQDCSCIQSL GNSSAVLGLC KKGPECANRL QYFLILTIII SFIYSLTAIP GYMVFLRCVK
541: SEEKSLGVGL HTFCIRVFAG IPAPVYFGAL IDRTCLHWGT LKCGQRGACR MYDINSFRHI
601: YLGLPIALRG SSYLPAFFIL ILMRKFQFPG DIDSSATDHT EMMLGEKESE HTDVHGSPQV
661: ENDGELKTKL