Demonstration of a common DPhe7 to DNal(2')7 peptide ligand antagonist switch for the melanocortin-3 and melanocortin-4 receptors identifies systematic mischaracterization of the pharmacological properties of melanocortin peptides
L. E. Gimenez, T. A. Noblin, S. Y. Williams, S. Mullick Bagchi, R.-L. Ji, Y.-X. Tao, C. B. Jeppesen, K. W. Conde-Frieboes, T. K. Sawyer, P. Grieco, R. D. Cone
The paper identifies a systematic mischaracterization of melanocortin peptide pharmacology by showing DNal(2)7 residues act as antagonists, not agonists, for MC3R and MC4R.
bioRxiv · Jan 3, 2022Pharmacology & Toxicology