AgRP-Derived melanocortin-5 receptor peptide antagonists
AgRP derived scaffolds composed of natural (Tyr, Ala, Val, Asn) and unnatural amino acids (Dap) with antagonist activity at the mouse MC5R
- Drug development
Melanocortin-5 receptor (MC5R) has been implicated in metabolic disorders, acne, inflammation, mental disorders and stress. However, the physiological functions of MC5R have not been clearly elucidated due to a lack of potent selective ligands. 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. This unique pharmacology has never been reported for this scaffold, and thus it could provide crucial therapeutic leads for drug development.
Phase of DevelopmentTRL: 2-3
A total of 5 compounds have been synthesized and evaluated for pharmacological activity in vitro.
Desired PartnershipsThis technology is now available for:
- Sponsored research
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- Koerperich, Z.M., Ericson, M.D., Freeman, K.T., Speth, R.C., Pogozheva, I.D., Mosberg, H.I. and Haskell-Luevano, C. (2019), Incorporation of agouti-related protein (AGRP) human single nucleotide polymorphisms (SNPs) in the AGRP-derived macrocyclic scaffold c [Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] decreases melanocortin-4 receptor antagonist potency and results in the discovery of melanocortin-5 receptor antagonists, Journal of medicinal chemistry
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