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Small Molecule Ligands of the Human Melanocortin-4 Receptor

[ Vol. 7 , Issue. 11 ]


Feroze Ujjainwalla and Iyassu K. Sebhat   Pages 1068 - 1084 ( 17 )


Genetic and pharmacological studies, involving both animals and humans, suggest that the central MC4 receptor plays a key role in homeostatic control, most probably via regulation of appetite and energy expenditure. This has stimulated intense research efforts in the field of drug discovery to identify MC4 receptor agonists and antagonists for the therapeutic treatment of obesity and diseases associated with loss of body weight. This article constitutes a near comprehensive review of the published scientific literature on small molecule ligands of the hMC4 receptor since 2002.


Computational modeling, cytochrome P450 3A4 isozyme, Piperidine, G-protein coupled receptors, MC4R Agonists


Department of Medicinal Chemistry, Merck Research Laboratories, Rahway NJ 07065-0900, USA.

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