Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016
Autor: | Mark D. Ericson, Katherine N. Schlasner, Cody J. Lensing, Skye R. Doering, Carrie Haskell-Luevano, Katlyn A. Fleming |
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Rok vydání: | 2017 |
Předmět: |
Models
Molecular 0301 basic medicine integumentary system Ligand Receptors Melanocortin digestive oral and skin physiology Computational biology Biology Ligands Combinatorial chemistry Article Melanocortins Small Molecule Libraries 03 medical and health sciences 030104 developmental biology 0302 clinical medicine Drug Discovery Animals Humans Molecular Medicine Amino Acid Sequence Melanocortin Molecular Biology hormones hormone substitutes and hormone antagonists 030217 neurology & neurosurgery |
Zdroj: | Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease. 1863:2414-2435 |
ISSN: | 0925-4439 |
DOI: | 10.1016/j.bbadis.2017.03.020 |
Popis: | 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. |
Databáze: | OpenAIRE |
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