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Hydroxycarboxylic acid-binding receptors
Stable Identifier
R-HSA-3296197
Type
Pathway
Species
Homo sapiens
ReviewStatus
5/5
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Signal Transduction (Homo sapiens)
Signaling by GPCR (Homo sapiens)
GPCR ligand binding (Homo sapiens)
Class A/1 (Rhodopsin-like receptors) (Homo sapiens)
Hydroxycarboxylic acid-binding receptors (Homo sapiens)
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The G-protein-coupled receptors Hydroxy-carboxylic acid receptor 1 (HCAR1, GPR81), HCAR2 (GPR109A), and HCAR3 (GPR109B) have significant sequence homology and are encoded by clustered genes. Their endogenous ligands are hydroxy-carboxylic acid metabolites. HCAR1 is activated by lactate (2-hydroxy-propanoic acid). HCAR2 is a receptor for 3-hydroxy-butyric acid. HCAR3 is activated by 3-hydroxy-octanoic acid. HCAR1 and HCAR2 are found in most mammalian species; HCA3 is found only in higher primates. All three receptors are expressed in adipocytes and are coupled to Gi-type G-proteins, mediating antilipolytic effects in fat cells. HCAR2 and HCAR3 are also expressed in a variety of immune cells. HCAR2 is a receptor for the antidyslipidemic drug nicotinic acid (niacin) and related natural and synthetic compounds.
Literature References
PubMed ID
Title
Journal
Year
21454438
International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B)
IJzerman, AP
,
Offermanns, S
,
Lovenberg, TW
,
Semple, G
,
Wise, A
,
Colletti, SL
Pharmacol. Rev.
2011
Participants
Events
HCAR2 binds HCAR2 ligands
(Homo sapiens)
HCAR1 binds LACT
(Homo sapiens)
HCAR3 binds HCAR3 ligands
(Homo sapiens)
Participates
as an event of
Class A/1 (Rhodopsin-like receptors) (Homo sapiens)
Orthologous Events
Hydroxycarboxylic acid-binding receptors (Bos taurus)
Hydroxycarboxylic acid-binding receptors (Canis familiaris)
Hydroxycarboxylic acid-binding receptors (Danio rerio)
Hydroxycarboxylic acid-binding receptors (Mus musculus)
Hydroxycarboxylic acid-binding receptors (Rattus norvegicus)
Hydroxycarboxylic acid-binding receptors (Sus scrofa)
Authored
Jupe, S (2013-04-17)
Created
Jupe, S (2013-04-18)
© 2025
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