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... [read more] acid (niacin), acipimox and acifran [1,2,3]. These receptors were provisionally described as nicotinic acid receptors, although nicotinic acid shows submicromolar potency at HCA₂receptors only and is unlikely to be the natural ligand [2,3].

References

Soga T, Kamohara M, Takasaki J, et al. Molecular identification of nicotinic acid receptor. Biochem Biophys Res Commun 2003;303:364-9.
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.
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.

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Human	HCAR1 hydroxycarboxylic acid receptor 1
Human	HCAR2 hydroxycarboxylic acid receptor 2
Human	HCAR3 hydroxycarboxylic acid receptor 3

Human

HCAR1

hydroxycarboxylic acid receptor 1

Human

HCAR2

hydroxycarboxylic acid receptor 2

Human

HCAR3

hydroxycarboxylic acid receptor 3

Species	Receptor	Family	Assays
Human	HCAR1 hydroxycarboxylic acid receptor 1	Hydroxycarboxylic acid receptors	Assay modes: - Panels: -	Reference agonist: EC50:
Human	HCAR2 hydroxycarboxylic acid receptor 2	Hydroxycarboxylic acid receptors	Available Assay modes: Agonist ⋅ Inverse agonist ⋅ Antagonist ⋅ PAM ⋅ NAM Panels: Human non-orphan GPCRs ⋅ Ophthalmology ⋅ Dermatology ⋅ à la carte	Reference agonist: nicotinic acid EC50: 5.8 µM
Human	HCAR3 hydroxycarboxylic acid receptor 3	Hydroxycarboxylic acid receptors	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

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