Hydroxycarboxylic acid receptors
Formerly known as: Nicotinic acid receptor family
More information on this family may be found on the IUPHAR-DB family and introduction pages.
The hydroxycarboxylic acid family of receptors (ENSFM00500000271913, nomenclature as agreed by NC-IUPHAR Subcommittee on Hydroxycarboxylic acid receptors, [5]) respond to organic acids, including the endogenous short chain fatty acids, butyric acid and L-lactic acid, as well as the lipid lowering agents nicotinic acid (niacin), acipimox and acifran [7,9-10]. These receptors were provisionally described as nicotinic acid receptors, although nicotinic acid shows submicromolar potency at HCA2 receptors only [9-10].
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Receptors 
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Boatman, PD; Richman, JG; Semple, G. (2008) Nicotinic acid receptor agonists. J. Med. Chem., 51 (24): 7653-62. [PMID:18983141]
Chapman, MJ; Redfern, JS; McGovern, ME; Giral, P. (2010) Niacin and fibrates in atherogenic dyslipidemia: pharmacotherapy to reduce cardiovascular risk. Pharmacol. Ther., 126 (3): 314-45. [PMID:20153365]
Gille, A; Bodor, ET; Ahmed, K; Offermanns, S. (2008) Nicotinic acid: pharmacological effects and mechanisms of action. Annu. Rev. Pharmacol. Toxicol., 48: 79-106. [PMID:17705685]
Guyton, JR. (2007) Niacin in cardiovascular prevention: mechanisms, efficacy, and safety. Curr. Opin. Lipidol., 18 (4): 415-20. [PMID:17620858]
Offermanns, S; Colletti, SL; Lovenberg, TW; Semple, G; Wise, A; IJzerman, AP. (2011) International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B). Pharmacol. Rev., 63 (2): 269-90. [PMID:21454438]
Soudijn, W; van Wijngaarden, I; Ijzerman, AP. (2007) Nicotinic acid receptor subtypes and their ligands. Med Res Rev, 27 (3): 417-33. [PMID:17238156]
Vosper, H. (2009) Niacin: a re-emerging pharmaceutical for the treatment of dyslipidaemia. Br. J. Pharmacol., 158 (2): 429-41. [PMID:19627285]
1. Ahmed, K; Tunaru, S; Langhans, CD; Hanson, J; Michalski, CW; Kölker, S; Jones, PM; Okun, JG; Offermanns, S. (2009) Deorphanization of GPR109B as a receptor for the beta-oxidation intermediate 3-OH-octanoic acid and its role in the regulation of lipolysis. J. Biol. Chem., 284 (33): 21928-33. [PMID:19561068]
2. Ahmed, K; Tunaru, S; Tang, C; Müller, M; Gille, A; Sassmann, A; Hanson, J; Offermanns, S. (2010) An autocrine lactate loop mediates insulin-dependent inhibition of lipolysis through GPR81. Cell Metab., 11 (4): 311-9. [PMID:20374963]
3. Cai, T.Q., Ren, N., Jin, L., Cheng, K., Kash, S., Chen, R., Wright, S.D., Taggart, A.K. and Waters, M.G. (2008) Role of GPR81 in lactate-mediated reduction of adipose lipolysis. Biochem Biophys Res Commun, 377 (3): 987-991. [PMID:18952058]
4. Liu, C., Wu, J., Zhu, J., Kuei, C., Yu, J., Shelton, J., Sutton, S.W., Li, X., Yun, S.J., Mirzadegan, T., Mazur, C., Kamme, F. and Lovenberg, T.W. (2009) Lactate Inhibits Lipolysis in Fat Cells through Activation of an Orphan G-protein-coupled Receptor, GPR81. J Biol Chem., 284 (5): 2811-2822. [PMID:19047060]
5. Offermanns, S; Colletti, SL; Lovenberg, TW; Semple, G; Wise, A; IJzerman, AP. (2011) International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B). Pharmacol. Rev., 63 (2): 269-90. [PMID:21454438]
6. Semple, G., Skinner, P. J., Cherrier, M. C., Webb, P. J., Sage, C. R., Tamura, S. Y., Chen, R., Richman, J. G. and Connolly, D. T. (2006) 1-Alkyl-benzotriazole-5-carboxylic acids are highly selective agonists of the human orphan G-protein-coupled receptor GPR109b. J Med Chem, 49: 1227-1230. [PMID:16480258]
7. Soga, T., Kamohara, M., Takasaki, J., Matsumoto, S., Saito, T., Ohishi, T., Hiyama, H., Matsuo, A., Matsushime, H. and Furuichi, K. (2003) Molecular identification of nicotinic acid receptor. Biochem Biophys Res Commun, 303: 364-369. [PMID:12646212]
8. Taggart, A. K., Kero, J., Gan, X., Cai, T. Q., Cheng, K., Ippolito, M., Ren, N., Kaplan, R., Wu, K., Wu, T. J., Jin, L., Liaw, C., Chen, R., Richman, J., Connolly, D., Offermanns, S., Wright, S. D. and Waters, M. G. (2005) (D)-beta-Hydroxybutyrate inhibits adipocyte lipolysis via the nicotinic acid receptor PUMA-G. J Biol Chem, 280: 26649-26652. [PMID:15929991]
9. Tunaru, S., Kero, J., Schaub, A., Wufka, C., Blaukat, A., Pfeffer, K. and Offermanns, S. (2003) PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect. Nat Med, 9: 352-355. [PMID:12563315]
10. Wise, A., Foord, S. M., Fraser, N. J., Barnes, A. A., Elshourbagy, N., Eilert, M., Ignar, D. M., Murdock, P. R., Steplewski, K., Green, A., Brown, A. J., Dowell, S. J., Szekeres, P. G., Hassall, D. G., Marshall, F. H., Wilson, S. and Pike, N. B. (2003) Molecular identification of high and low affinity receptors for nicotinic acid. J Biol Chem, 278: 9869-9874. [PMID:12522134]
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Further closely-related GPCR include the 5-oxoeicosanoid receptor (ENSG00000162881) and GPR31 (ENSG00000120436).