Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors
- PMID: 15876475
- DOI: 10.1016/j.peptides.2005.03.020
Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors
Abstract
alpha-MSH and gamma-MSH are the natural endogenous hormones for the human melanocortin-1, 3, 4 and 5 receptors (hMC1R, hMC3R, hMC4R and hMC5R). These and more potent, stable and prolonged acting analogues such as NDP-alpha-MSH, MT-II and SHU-9119 are not very receptor selective. To develop potent and selective agonist and antagonist ligands for the melanocortin receptors we have used state-of-the-art biophysical studies, computational chemistry, and design of conformational and topographical constraints with novel templates.
Similar articles
-
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.J Med Chem. 1997 May 23;40(11):1738-48. doi: 10.1021/jm960845e. J Med Chem. 1997. PMID: 9171884
-
Design and synthesis of highly potent and selective melanotropin analogues of SHU9119 modified at position 6.Biochem Biophys Res Commun. 2002 Apr 12;292(4):1075-80. doi: 10.1006/bbrc.2002.6739. Biochem Biophys Res Commun. 2002. PMID: 11944925
-
Structure-activity relationships of gamma-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. Discovery of highly selective hMC3R, hMC4R, and hMC5R analogues.J Med Chem. 2003 Nov 6;46(23):4965-73. doi: 10.1021/jm030119t. J Med Chem. 2003. PMID: 14584947
-
Overview of endogenous and synthetic melanocortin peptides.Cell Mol Biol (Noisy-le-grand). 2006 May 30;52(2):3-20. Cell Mol Biol (Noisy-le-grand). 2006. PMID: 16914082 Review.
-
Melanocortin ligands: 30 years of structure-activity relationship (SAR) studies.Med Res Rev. 2004 May;24(3):325-56. doi: 10.1002/med.10064. Med Res Rev. 2004. PMID: 14994367 Review.
Cited by
-
Alpha-melanocyte-stimulating hormone (αMSH) modulates the rewarding properties of social interactions in an oxytocin receptor-dependent manner in Syrian hamsters (Mesocricetus Auratus).Physiol Behav. 2022 Aug 1;252:113828. doi: 10.1016/j.physbeh.2022.113828. Epub 2022 Apr 30. Physiol Behav. 2022. PMID: 35500727 Free PMC article.
-
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.J Med Chem. 2006 Nov 16;49(23):6888-96. doi: 10.1021/jm060768f. J Med Chem. 2006. PMID: 17154518 Free PMC article.
-
Tackling obesity: new therapeutic agents for assisted weight loss.Diabetes Metab Syndr Obes. 2010 Apr 26;3:95-112. Diabetes Metab Syndr Obes. 2010. PMID: 21437080 Free PMC article.
-
Solid-phase peptide head-to-side chain cyclodimerization: discovery of C(2)-symmetric cyclic lactam hybrid α-melanocyte-stimulating hormone (MSH)/agouti-signaling protein (ASIP) analogues with potent activities at the human melanocortin receptors.Peptides. 2010 Oct;31(10):1894-905. doi: 10.1016/j.peptides.2010.06.026. Epub 2010 Aug 3. Peptides. 2010. PMID: 20688117 Free PMC article.
-
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.Bioorg Med Chem Lett. 2011 May 15;21(10):3099-102. doi: 10.1016/j.bmcl.2011.03.019. Epub 2011 Mar 13. Bioorg Med Chem Lett. 2011. PMID: 21486697 Free PMC article.
Publication types
MeSH terms
Substances
Grants and funding
LinkOut - more resources
Full Text Sources
Other Literature Sources