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SLCO family of organic anion transporting polypeptides C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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The SLCO superfamily is comprised of the organic anion transporting polypeptides (OATPs). The 11 human OATPs are divided into 6 families and ten subfamilies based on amino acid identity. These proteins are located on the plasma membrane of cells throughout the body. They have 12 TM domains and intracellular termini, with multiple putative glycosylation sites. OATPs mediate the sodium-independent uptake of a wide range of amphiphilic substrates, including many drugs and toxins. Due to the multispecificity of these proteins, this guide lists classes of substrates and inhibitors for each family member. More comprehensive lists of substrates, inhibitors, and their relative affinities may be found in the review articles listed below.

Transporters

1220
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OATP1A2 / SLCO1A2 C Show summary »

OATP1B1 / SLCO1B1 C Show summary »


Target Id 1220
Nomenclature OATP1B1
Systematic nomenclature SLCO1B1
Previous and unofficial names solute carrier organic anion transporter family, member 1B1
Genes SLCO1B1 (Hs)
Ensembl ID ENSG00000134538 (Hs)
UniProtKB AC Q9Y6L6 (Hs)
Bioparadigms SLC Tables SLCO1B1 (Hs)
Endogenous substrates
bilirubin
bile acids
leukotrienes
steroid conjugates
thyroid hormones
Substrates
rifampicin
bromsulphthalein
fexofenadine
ACE inhibitors
anticancer drugs
antifungals
β-lactam antibiotics
bile acid derivatives and conjugates
endothelin receptor antagonists
HIV protease inhibitors
opioids
sartans
statins
Ligands
pravastatin (Binding)
Inhibitors
cyclosporin A pKi 7.3 [3,7]
rifampicin pKi 6.0 [7]
rifamycin SV pKi 5.7 [10]
estrone-3-sulphate pIC50 7.2 [5]
gemfibrozil [8]
glycyrrhizin
indocyanine green
Labelled ligands
[3H]estradiol-17β-glucuronide
[3H]estrone-3-sulphate
Comment Other inhibitors include, fibrates, flavonoids, glitazones and macrolide antibiotics. Estrone-3-sulphate or the drug substrates atorvastatin, pravastatin and rosuvastatin are used as a probe.

OATP1B3 / SLCO1B3 C Show summary »

OATP1C1 / SLCO1C1 C Show summary »

OATP2A1 / SLCO2A1 C Show summary »

OATP2B1 / SLCO2B1 C Show summary »

OATP3A1 / SLCO3A1 C Show summary »

OATP4A1 / SLCO4A1 C Show summary »

OATP4C1 / SLCO4C1 C Show summary »

OATP5A1 / SLCO5A1 Show summary »

OATP6A1 / SLCO6A1 Show summary »

Further reading

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: Transporters. Br J Pharmacol. 176 Issue S1: S397-S493.