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

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  Shi, Qing, Ornstein, Paul L., Briner, Karin, Richardson, Timothy   I., Arnold, Macklin B., Backer, Ryan T., Buckmaster, Jennifer L.,   Canada, Emily J., Doecke, Christopher W., Hertel, Larry W.,   Honigschmidt, Nick, Hsiung, Hansen M., Husain, Saba, Kuklish,   Steve L., Martinelli, Michael J., Mullaney, Jeffrey T., O'Brien,   Thomas P., Reinhard, Matt R., Rothhaar, Roger, Shah, Jikesh, Wu,   Zhipei, Xie, Chaoyu, Zgombick, John M., Fisher, Matthew J.   Bioorganic & Medicinal Chemistry Letters  2006 16 (9) 2341-2346

  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. (C) 2005 Elsevier Ltd.   All rights reserved.

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