Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties

  • J Med Chem. 2003 Mar 27;46(7):1123-6. doi: 10.1021/jm025600i.
Timothy F Herpin  1 ,  Guixue Yu ,  Kenneth E Carlson ,  George C Morton ,  Ximao Wu ,  Liya Kang ,  Huji Tuerdi ,  Ashish Khanna ,  John S Tokarski ,  R Michael Lawrence ,  John E Macor
Affiliations
  • 1. Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 5400, Princeton, New Jersey 08543, USA.
PMID: 12646021 DOI: 10.1021/jm025600i
Abstract

The melanocortin-1 receptor (MC-1R) is a G-protein-coupled receptor involved in inflammation and skin pigmentation. Compound 2 is the first highly potent and selective MC-1R small-molecule agonist reported. Compound 2 showed efficacy in an acute model of inflammation, which has demonstrated the role of MC-1R in modulation of inflammation.

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