Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists |
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Authors: | Liu Xue-Wei Ma Jimei Colson Anny-Odile Doersen Doreen Cross Ebetino Frank H |
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Institution: | Division of Chemistry and Biological Chemistry, School of Physical and Mathematical Sciences, Nanyang Technological University, Singapore 637371, Singapore. xuewei@ntu.edu.sg |
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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. |
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