Hydroxycarboxylic Acid Receptor 1 Antibodies

The hydroxycarboxylic acid receptor 1 (HCA1), also known as GPR81, is a class A G protein-coupled receptor that is primarily activated by the endogenous metabolite lactate and plays an important role in metabolic regulation. Pharmacologically, no widely approved drugs selectively target HCA1, although experimental agonists and modulators are being investigated for potential applications in metabolic and inflammatory diseases. Upon ligand binding, HCA1 predominantly couples to Gi/o proteins, leading to inhibition of adenylate cyclase, reduced intracellular cyclic AMP levels, and suppression of lipolysis in adipocytes. This signaling mechanism links cellular energy status and lactate production to systemic lipid metabolism and metabolic homeostasis. Additional downstream effects may involve modulation of MAP kinase pathways and regulation of gene expression related to inflammation and tissue protection. HCA1 is highly expressed in adipose tissue, particularly in adipocytes, but is also detected in skeletal muscle, liver, brain, and certain immune cells. The distribution and signaling properties of HCA1 highlight its emerging relevance as a metabolic sensor and a potential therapeutic target in disorders such as obesity, insulin resistance, and inflammatory disease. For more information on HCA1 receptor pharmacology please refer to the IUPHAR database. For further reading refer to:

Offermanns S, Colletti SL, Lovenberg TW, Semple G, Wise A, IJzerman AP. International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B). Pharmacol Rev. 2011 Jun;63(2):269-90. doi: 10.1124/pr.110.003301. Epub 2011 Mar 31. PMID: 21454438.

Colletti SL, IJzerman AP, Lovenberg TW, Offermanns S, Semple G, Waters MG, Wise A. Hydroxycarboxylic acid receptors in GtoPdb v.2023.1. IUPHAR/BPS Guide to Pharmacology CITE. 2023; 2023(1).