Novel pharmacological MC4R agonists can efficiently activate mutated MC4R from obese patient with impaired endogenous agonist response.

@article{Roubert2010NovelPM,
  title={Novel pharmacological MC4R agonists can efficiently activate mutated MC4R from obese patient with impaired endogenous agonist response.},
  author={Pierre Roubert and B{\'e}atrice Dubern and P. S. C. Van Der Plas and C{\'e}cile Lubrano-Berthelier and Rohia Alihi and Florence Auger and Daniel deOliveira and Jesse Z Dong and Arnaud Basdevant and Christophe Thurieau and Karine Cl{\'e}ment},
  journal={The Journal of endocrinology},
  year={2010},
  volume={207 2},
  pages={177-83}
}
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 hMC4R mutations chosen based on the nature of their functional alterations, i.e… CONTINUE READING
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Melanocortin receptor ligands modified with hydantoin. International patent WO 2008/147556

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  • 2008
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