title: Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists.
abstract: A series of novel peptidomimetic analogs was prepared containing cyclohexyl, phenyl, or heterocyclic groups to ostensibly orient the guanidine or mimic of an arginine in a putative melanocortin receptor ligand pharmacophore. Some binding affinity at the melanocortin receptors MC(3) and MC(4) was noted. In silico docking also indicated that the relative positions of the hydrogen-bonding sites and hydrophobic regions of the compounds are reasonably well matched to the receptor-binding site. This may present a lead entry into a selective series of MC(4)R agonists.
authors: Division of Chemistry and Biological Chemistry, School of Physical and Mathematical Sciences, Nanyang Technological University, Singapore 637371, Singapore. xuewei@ntu.edu.sg
authors: Xue-Wei
authors: XW
authors: Liu
authors: Jimei
authors: J
authors: Ma
authors: Anny-Odile
authors: AO
authors: Colson
authors: Doreen Cross
authors: DC
authors: Doersen
authors: Frank H
authors: FH
authors: Ebetino
mesh_terms: D001120:Arginine / Q000737:chemistry; D006146:Guanidines / Q000737:chemistry; D006801:Humans; D008954:Models, Biological; D018716:Molecular Mimicry; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry*; D044104:Receptor, Melanocortin, Type 3 / Q000819:agonists*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D006146:Guanidines; D010455:Peptides; D044104:Receptor, Melanocortin, Type 3; D044105:Receptor, Melanocortin, Type 4; D014230:Triazoles; D001120:Arginine