Journal
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
Volume 1863, Issue 10, Pages 2414-2435Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.bbadis.2017.03.020
Keywords
Selective ligands; Small molecules; Sexual dimorphism; Bivalent/multivalent ligands; Clinical trials
Funding
- NIH [R01DK108893, R01DK091906, R01DK097838]
- NIH Postdoctoral Fellowship [F32DK108402]
- Olsteins Graduate Fellowship from University of Minnesota
- Doctoral Dissertation Fellowship from University of Minnesota
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The discovery of the endogenous melanocortin agonists in the 1950s have resulted in sixty years of melanocortin ligand research. Early efforts involved truncations or select modifications of the naturally occurring agonists leading to the development of many potent and selective ligands. With the identification and cloning of the five known melanocortin receptors, many ligands were improved upon through bench-top in vitro assays. Optimization of select properties resulted in ligands adopted as clinical candidates. A summary of every melanocortin ligand is outside the scope of this review. Instead, this review will focus on the following topics: classic melanocortin ligands, selective ligands, small molecule (non-peptide) ligands, ligands with sex-specific effects, bivalent and multivalent ligands, and ligands advanced to clinical trials. Each topic area will be summarized with current references to update the melanocortin field on recent progress. This article is part of a Special Issue entitled: Melanocortin Receptors - edited by Ya-Xiong Tao.
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