Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity

  • ACS Med Chem Lett. 2010 Oct 18;2(1):43-7. doi: 10.1021/ml100196d.
Iyassu K Sebhat  1 ,  Christopher Franklin  1 ,  Michael M-C Lo  1 ,  David Chen  1 ,  James P Jewell  1 ,  Randy Miller  2 ,  Jianmei Pang  2 ,  Oksana Palyha  3 ,  Yanqing Kan  3 ,  Theresa M Kelly  3 ,  Xiao-Ming Guan  3 ,  Donald J Marsh  3 ,  Jennifer A Kosinski  3 ,  Joseph M Metzger  4 ,  Kathryn Lyons  2 ,  Jasminka Dragovic  2 ,  Peter R Guzzo  5 ,  Alan J Henderson  5 ,  Marc L Reitman  3 ,  Ravi P Nargund  1 ,  Matthew J Wyvratt  1 ,  Linus S Lin  1
Affiliations
  • 1. Departments of Medicinal Chemistry.
  • 2. Drug Metabolism.
  • 3. Metabolic Diseases (Obesity).
  • 4. Pharmacology.
  • 5. AMRI, 26 Corporate Circle, Albany, New York 12212, United States.
PMID: 24900253 DOI: 10.1021/ml100196d
Abstract

We report the development and characterization of compound 22 (MK-5046), a potent, selective small molecule agonist of BRS-3 (Bombesin Receptor subtype-3). In pharmacological testing using diet-induced obese mice, compound 22 caused mechanism-based, dose-dependent reductions in food intake and body weight.

Keywords
MK-5046; bombesin receptor subtype-3 agonist; obesity.
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