Article
Novel pharmacological MC4R agonists can efficiently activate mutated MC4R from obese patient with impaired endogenous agonist response.
The Journal of endocrinology - 1 Nov 2010
Roubert Pierre, Dubern Béatrice, Plas Pascale, Lubrano-Berthelier Cécile, Alihi Rohia, Auger Florence, Deoliveira Daniel B, Dong Jesse Z, Basdevant Arnaud, Thurieau Christophe, Clément Karine
Abstract excerpt
Human melanocortin 4 receptor (hMC4R) mutations with in vitro functional effects are responsible for 0.5-2.5% of severe obesity. Designing ligands that are able to counteract this in vitro-associated molecular defect is crucial to develop specific anti-obesity drugs in these genetically associated cases. We analyzed the in vitro effect of two novel melanocortin agonists, IRC-022493 and IRC-022511, on typical...
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