Hydroxycarboxylic acid receptors

Overview

The hydroxycarboxylic acid family of receptors respond to organic acids, including the endogenous hydroxy carboxylic acids 3-hydroxy butyric acid and L-lactic acid, as well as the lipid lowering agents nicotinic acid (niacin), acipimox and acifran [1,2,3]. These receptors were provisionally described as nicotinic acid receptors, although nicotinic acid shows submicromolar potency at HCA2 receptors only and is unlikely to be the natural ligand [2,3].

References

  1. Soga T, Kamohara M, Takasaki J, et al. Molecular identification of nicotinic acid receptor. Biochem Biophys Res Commun 2003;303:364-9.
  2. Tunaru S, Kero J, Schaub A, et al. PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect. Nat Med 2003;9:352-5.
  3. Wise A, Foord SM, Fraser NJ, et al. Molecular identification of high and low affinity receptors for nicotinic acid. J Biol Chem 2003;278:9869-74.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Assay modes:
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Reference agonist:
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Human
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Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
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Human non-orphan GPCRs
Ophthalmology
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Reference agonist:
nicotinic acid
EC50:
5.8 µM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Dermatology
à la carte
Reference agonist:
3‐OH‐octanoic acid
EC50:
130 µM