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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

1221
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OATP1A2 / SLCO1A2 C Show summary »

OATP1B1 / SLCO1B1 C Show summary »

OATP1B3 / SLCO1B3 C Show summary »


Target Id 1221
Nomenclature OATP1B3
Systematic nomenclature SLCO1B3
Previous and unofficial names LST-2 | OATP8 | SLC21A8 | solute carrier family 21 (organic anion transporter), member 8 | liver-specific organic anion transporter 1 | solute carrier organic anion transporter family, member 1B3
Genes SLCO1B3 (Hs)
Ensembl ID ENSG00000111700 (Hs)
UniProtKB AC Q9NPD5 (Hs)
Bioparadigms SLC Tables SLCO1B3 (Hs)
Endogenous substrates
CCK-8
LTC4
bilirubin
bile acids
steroid conjugates
thyroid hormones
Substrates
erythromycin
rifampicin
bromsulphthalein
amanitin
digoxin
phalloidin
saquinavir
fexofenadine
ouabain
anticancer drugs
β-lactam antibiotics
bile acid derivatives and conjugates
opioids
sartans
statins
Inhibitors
cyclosporin A pIC50 6.1 [7,9]
sildenafil pIC50 6.1 [9]
rifampicin pIC50 5.8 [7,9]
gemfibrozil
rifamycin SV
glycyrrhizin
Labelled ligands
[3H]BSP
[3H]estradiol-17β-glucuronide
[3H]CCK-8 (human, mouse, rat)
Comment Other inhibitors include, HIV protease inhibitors, glitazones and macrolide antibiotics. CCK-8 is used as an OATP1B3-selective probe.

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.