Chemistry:GSK256073
From HandWiki
GSK256073 is an experimental drug which acts as a potent and selective agonist for the Hydroxycarboxylic acid receptor 2 (GPR109A). It reduces blood sugar levels and was trialed unsuccessfully as a potential treatment for diabetes, but continues to be used for research into the function of the HCA2 receptor.[1][2][3][4][5]
References
- ↑ "GSK256073, a selective agonist of G-protein coupled receptor 109A (GPR109A) reduces serum glucose in subjects with type 2 diabetes mellitus". Diabetes, Obesity & Metabolism 15 (11): 1013–1021. November 2013. doi:10.1111/dom.12132. PMID 23701262.
- ↑ "GSK256073 acutely regulates NEFA levels via HCA2 agonism but does not achieve durable glycaemic control in type 2 diabetes. A randomised trial". European Journal of Pharmacology 755: 95–101. May 2015. doi:10.1016/j.ejphar.2015.03.005. PMID 25773496.
- ↑ "Discovery and characterization of GSK256073, a non-flushing hydroxy-carboxylic acid receptor 2 (HCA2) agonist". European Journal of Pharmacology 756: 1–7. June 2015. doi:10.1016/j.ejphar.2015.01.051. PMID 25773497.
- ↑ "Molecular recognition of niacin and lipid-lowering drugs by the human hydroxycarboxylic acid receptor 2". Cell Reports 42 (11). November 2023. doi:10.1016/j.celrep.2023.113406. PMID 37952153.
- ↑ "The hydroxycarboxylic acid receptor HCA2 is required for the protective effect of ketogenic diet in epilepsy". Pharmacology Research & Perspectives 12 (6). December 2024. doi:10.1002/prp2.70026. PMID 39439218.
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