To better define the role of MC5R in pathophysiology and also to develop novel therapeutic modalities targeting MC5R, it is imperative to develop synthetic agonists and antagonists of MC5R with improved specificity.

The modification of pharmacophores (Arg-Phe-Phe-Asn-Ala-Phe) on exposed β-hairpin loops of AgRP or ASIP can improve the antagonist potency or cause a functional change from an antagonist to an inverse agonist for MC5R.

Oct 10, 2017 · In this study, the Asn and Ala positions of a reported AGRP macrocyclic scaffold (c [Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro]) were explored with 14-compound and 8-compound libraries, respectively, to generate more potent, selective melanocortin receptor antagonists.

Mar 25, 2025 · Anti-MC5 Receptor Antibody from Alomone Labs is a highly specific rabbit polyclonal Ab directed against an epitope of the mouse MC5R. Applications: IHC, WB. Free samples available.

While the melanocortin receptors (MCRs) are known to be involved in numerous biological pathways, the potential roles of the MC5R have not been clearly elucidated in humans. AgRP, an MC3R/MC4R antagonist and MC4R inverse agonist, contains an exposed ...

Mar 12, 2020 · Agouti-related protein (AgRP), an MC3R/MC4R antagonist and MC4R inverse agonist, contains an exposed β-hairpin loop composed of six residues (Arg-Phe-Phe-Asn-Ala-Phe) that is imperative for binding and function.

It shows genes and PPIs with information about pathways, protein-protein interactions (PPIs), Gene Ontology (GO) annotations including cellular localization, molecular function and biological process, drugs, diseases, genome-wide association studies (GWAS), GO enrichments, PDB ID, Uniprot ID, HPRD ID, and word cloud from pubmed abstracts.

This novel technology consists of five compounds that have antagonist activity (sub-micromolar) at the mouse MC5R. The proposed compounds are chemical scaffolds derived from agouti-related protein (AgRP), which is an endogenous antagonist for the melanocortin receptor family.

The central melanocortin (MC) system has been demonstrated to act downstream of leptin in the regulation of body weight. The system comprises alpha-MSH, which acts as agonist, and agouti-related protein (AgRP), which acts as antagonist at the …

Two endogenous antagonists [agouti related protein (AGRP) and agouti ] have been discovered to antagonize the centrally expressed MC3R and MC4Rs. All the endogenous agonists share a common His-Phe-Arg-Trp (6–9; α-MSH numbering) pharmacophore domain in their primary amino acid sequence.