Description
Title: Beyond Melanocyte-Stimulating Hormones and Adrenocorticotropin, Ligands for Melanocortin Receptors
Abstract: Over 100 years of study on melanocortins have been conducted since their discovery in 1916. Numerous studies have clarified the well-known roles that melanocortins play in the body that are mediated by cell surface receptors like the MSHR (melanocyte-stimulating hormone receptor) and ACTHR (adrenocorticotropin receptor). Three more melanocortin receptors (MCRs) were later discovered. Among these five MCRs, MC3R and MC4R are known as the neural MCRs because they are primarily expressed in the central nervous system. Targeting neural MCRs is emerging as a therapeutic strategy for treating metabolic conditions like obesity and cachexia because the central melanocortin system plays significant roles in regulating energy homeostasis. Many powerful and specific ligands were created early on as a result of modifications made to endogenous ligands. This review focuses on the ligands for neural MCRs, which include clinically approved ligands, nonclassical ligands, and classical ligands (MSH and agouti-related peptide), as well as small molecules, pharmacoperones, lipocalin 2, and -defensin (ACTH, setmelanotide, bremelanotide, and several repurposed drugs).
Keywords: neural melanocortin receptors; obesity; small molecule; pharmacoperone; drug
repurposing
Paper Quality: SCOPUS / Web of Science Level Research Paper
Subject: Biomolecules
Writer Experience: 20+ Years
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