Biology:SLCO1B3
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Solute carrier organic anion transporter family member 1B3 (SLCO1B3) also known as organic anion-transporting polypeptide 1B3 (OATP1B3) is a protein that in humans is encoded by the SLCO1B3 gene.[1]
OATP1B3 is a 12-transmembrane domain influx transporter. Normally expressed in the liver, the transporter functions to uptake large, non-polar drugs and hormones from the portal vein.
Clinical significance
OATP1B3 has also been identified as a transporter aberrantly expressed in prostate cancer and implicated in prostate cancer progression.[2] Increasing mRNA expression of OATP1B3 was also correlated to prostate cancer Gleason score.[3]
In addition, lower expression of OATP1B3 mRNA was also detected in testicular cancer.[3]
Substrates
Small molecules that are transported by SLCO1B3 include:[4]
- Amanitin
- Atrasentan
- Bilirubin
- Bosentan
- BQ-123
- Bromsulphthalein (BSP)
- CDCA-NBD
- Cholate (CA)
- Cholecystokinin octapeptide (CCK-8)
- Dehydroepiandroserone-3-sulfate (DHEAS)
- Deltorphin II
- Demethylphalloin
- Digoxin
- Docetaxel
- [D-penicillamine2,5]enkephalin (DPDPE)
- Enalapril
- Estradiol-17β-glucuronide 5–25
- Estrone-3-sulfate
- Fexofenadine
- Fluvastatin
- Fluo-3
- Glutathione (GSH)
- Glycocholate (GCA)
- Glycoursodeoxycholate (GUDCA)
- Irinotecan
- Leukotriene C4 (LTC4)
- Methotrexate
- Microcystin
- Monoglyucuronosyl
- Olmesartan
- Ouabain
- Paclitaxel
- Phalloidin
- Pitavastatin
- Rifampicin
- Ro 48-5033 (Bosentan metabolite)
- Rosuvastatin
- SN-38
- Taurocholate (TCA)
- Taurochenodeoxycholate (TCDCA)
- Taurodeoxycholate (TDCA)
- Tauroursodeoxycholate (TUDCA)
- Telmisartan
- Thyroxine (T4)
- TR-14035
- Triiodothyronine (T3)
- Valsartan
See also
References
- ↑ "Entrez Gene: SLCO1B3 solute carrier organic anion transporter family, member 1B3". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=28234.
- ↑ "Effect of SLCO1B3 haplotype on testosterone transport and clinical outcome in caucasian patients with androgen-independent prostatic cancer". Clin. Cancer Res. 14 (11): 3312–8. June 2008. doi:10.1158/1078-0432.CCR-07-4118. PMID 18519758.
- ↑ 3.0 3.1 Heather Pressler; Tristan M. Sissung; David Venzon; Douglas K. Price; William D. Figg (May 2011). "Expression of OATP Family Members in Hormone-Related Cancers: Potential Markers of Progression". Clin. Cancer Res. 6 (5): e20372. doi:10.1371/journal.pone.0020372. PMID 21625523. PMC 3098289. http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0020372.
- ↑ "Xenobiotic transporters of the human organic anion transporting polypeptides (OATP) family". Xenobiotica 38 (7–8): 778–801. July 2008. doi:10.1080/00498250801986951. PMID 18668430.
Further reading
- "Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide". J. Biol. Chem. 275 (30): 23161–8. 2000. doi:10.1074/jbc.M001448200. PMID 10779507.
- "LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers". Gastroenterology 120 (7): 1689–99. 2001. doi:10.1053/gast.2001.24804. PMID 11375950.
- "Hepatic uptake of cholecystokinin octapeptide by organic anion-transporting polypeptides OATP4 and OATP8 of rat and human liver". Gastroenterology 121 (5): 1185–90. 2001. doi:10.1053/gast.2001.28704. PMID 11677211.
- "Human organic anion transporting polypeptide 8 promoter is transactivated by the farnesoid X receptor/bile acid receptor". Gastroenterology 122 (7): 1954–66. 2002. doi:10.1053/gast.2002.33583. PMID 12055601.
- "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. 2003. doi:10.1073/pnas.242603899. PMID 12477932.
- "Detection of the human organic anion transporters SLC21A6 (OATP2) and SLC21A8 (OATP8) in liver and hepatocellular carcinoma". Lab. Invest. 83 (4): 527–38. 2003. doi:10.1097/01.lab.0000065015.02412.48. PMID 12695556.
- "Complete sequencing and characterization of 21,243 full-length human cDNAs". Nat. Genet. 36 (1): 40–5. 2004. doi:10.1038/ng1285. PMID 14702039.
- "The human organic anion transporting polypeptide 8 (SLCO1B3) gene is transcriptionally repressed by hepatocyte nuclear factor 3beta in hepatocellular carcinoma". J. Hepatol. 40 (2): 212–8. 2004. doi:10.1016/j.jhep.2003.10.008. PMID 14739090.
- "Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans". J. Pharmacol. Exp. Ther. 311 (1): 139–46. 2004. doi:10.1124/jpet.104.068056. PMID 15159445.
- "Mutations in the SLCO1B3 gene affecting the substrate specificity of the hepatocellular uptake transporter OATP1B3 (OATP8)". Pharmacogenetics 14 (7): 441–52. 2005. doi:10.1097/01.fpc.0000114744.08559.92. PMID 15226676.
- "Transport of fluorescent chenodeoxycholic acid via the human organic anion transporters OATP1B1 and OATP1B3". J. Lipid Res. 47 (6): 1196–202. 2006. doi:10.1194/jlr.M500532-JLR200. PMID 16534140.
- "Farnesoid X receptor, hepatocyte nuclear factors 1alpha and 3beta are essential for transcriptional activation of the liver-specific organic anion transporter-2 gene". J. Gastroenterol. 41 (4): 369–77. 2006. doi:10.1007/s00535-006-1784-3. PMID 16741617.
- "OATP8/1B3-mediated cotransport of bile acids and glutathione: an export pathway for organic anions from hepatocytes?". J. Biol. Chem. 281 (41): 30326–35. 2006. doi:10.1074/jbc.M602048200. PMID 16877380.
- "Human organic anion transporter 1B1 and 1B3 function as bidirectional carriers and do not mediate GSH-bile acid cotransport". Am. J. Physiol. Gastrointest. Liver Physiol. 293 (1): G271–8. 2007. doi:10.1152/ajpgi.00075.2007. PMID 17412826.
- "Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil". Drug Metab. Dispos. 35 (8): 1400–7. 2007. doi:10.1124/dmd.106.013615. PMID 17496208.
- "Human liver-specific organic anion transporter-2 is a potent prognostic factor for human breast carcinoma". Cancer Sci. 98 (10): 1570–6. 2007. doi:10.1111/j.1349-7006.2007.00570.x. PMID 17760952.
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