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Current Mechanistic and Pharmacodynamic Understanding of Melanocortin-4 Receptor Activation

Rhythm Pharmaceuticals, Boston, MA 02116, USA
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Academic Editors: Henry Mosberg, Tomi Sawyer and Carrie Haskell-Luevano
Molecules 2019, 24(10), 1892; https://doi.org/10.3390/molecules24101892
Received: 21 April 2019 / Revised: 15 May 2019 / Accepted: 15 May 2019 / Published: 16 May 2019
PDF [361 KB, uploaded 16 May 2019]

Abstract

In this work we summarize our understanding of melanocortin 4 receptor (MC4R) pathway activation, aiming to define a safe and effective therapeutic targeting strategy for the MC4R. Delineation of cellular MC4R pathways has provided evidence for distinct MC4R signaling events characterized by unique receptor activation kinetics. While these studies remain narrow in scope, and have largely been explored with peptidic agonists, the results provide a possible correlation between distinct ligand groups and differential MC4R activation kinetics. In addition, when a set of small-molecule and peptide MC4R agonists are compared, evidence of biased signaling has been reported. The results of such mechanistic studies are discussed.
Keywords: melanocortin-4 receptor; obesity; peptide agonist; cardiovascular profile; GαS signaling; receptor desensitization; receptor internalization melanocortin-4 receptor; obesity; peptide agonist; cardiovascular profile; GαS signaling; receptor desensitization; receptor internalization
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Sharma, S.; Garfield, A.S.; Shah, B.; Kleyn, P.; Ichetovkin, I.; Moeller, I.H.; Mowrey, W.R.; Van der Ploeg, L.H. Current Mechanistic and Pharmacodynamic Understanding of Melanocortin-4 Receptor Activation. Molecules 2019, 24, 1892.

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