Identification of arginine analogues as antagonists and agonists for the melanocortin-4 receptor

…, T Okubo, S Chaki, S Okuyama, A Nakazato

Index: Nozawa, Dai; Okubo, Taketoshi; Chaki, Shigeyuki; Okuyama, Shigeru; Nakazato, Atsuro Chemical and Pharmaceutical Bulletin, 2007 , vol. 55, # 8 p. 1232 - 1239

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Citation Number: 3

Abstract

In the present study, conducted to explore potent and small molecular melanocortin-4 (MC4) receptor ligands, we found that tripeptide 3a, containing a D-Phe-Arg-2-Nal (Nal; naphthylalanine) sequence, exhibited a moderate affinity for the MC4 receptor. Structural optimization led to the identification of a compound with a high affinity for the MC4 receptor, namely, tripeptide 3e, which showed a 70-fold higher affinity for the MC4 receptor than the ...