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1. Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor.

Author

Shi Q, Ornstein PL, Briner K, Richardson TI, Arnold MB, Backer RT, Buckmaster JL, Canada EJ, Doecke CW, Hertel LW, Honigschmidt N, Hsiung HM, Husain S, Kuklish SL, Martinelli MJ, Mullaney JT, O'Brien TP, Reinhard MR, Rothhaar R, Shah J, Wu Z, Xie C, Zgombick JM, and Fisher MJ

Subjects
Dipeptides chemistry, Ligands, Molecular Structure, Piperazines chemistry, Protein Binding, Receptor, Melanocortin, Type 4 chemistry, Stereoisomerism, Structure-Activity Relationship, Dipeptides chemical synthesis, Dipeptides pharmacology, Receptor, Melanocortin, Type 4 drug effects
Abstract

A series of benzylic piperazines (e.g., 4 and 5) attached to an 'address element', the dipeptide H-D-Tic-D-p-Cl-Phe-OH, 3 has been identified as ligands for the melanocortin subtype-4 receptor (MC4R). We describe herein the structure-activity relationship (SAR) studies on the N-terminal residue of the 'address element'. Several novel dipeptides and reduced dipeptides with high MC4R binding affinities and selectivity emerged from this SAR study.

Published
2006
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