Xiao Ming Guan

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. doi request reprint Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist
    Xiao Ming Guan
    Department of Metabolic Disorders, Merck Research Laboratories, Rahway, New Jersey 07065 0900, USA
    J Pharmacol Exp Ther 336:356-64. 2011
  2. doi request reprint Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity
    Jian Liu
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 20:2074-7. 2010
  3. doi request reprint Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity
    Xiao Ming Guan
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Cell Metab 11:101-12. 2010
  4. doi request reprint Body temperature as a mouse pharmacodynamic response to bombesin receptor subtype-3 agonists and other potential obesity treatments
    Joseph M Metzger
    Departments of Pharmacology, Rahway, NJ 07065, USA
    Am J Physiol Endocrinol Metab 299:E816-24. 2010
  5. pmc Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism
    Donald J Marsh
    Department of Obesity Research, Animal Pharmacology, and Comparative Medicine, Merck Research Laboratories, Rahway, NJ 07065, USA
    Proc Natl Acad Sci U S A 99:3240-5. 2002
  6. doi request reprint The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization
    Harry R Chobanian
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem 20:2845-9. 2012
  7. doi request reprint Bombesin receptor subtype-3 (BRS-3) regulates glucose-stimulated insulin secretion in pancreatic islets across multiple species
    Yue Feng
    Department of Diabetes and Obesity, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Endocrinology 152:4106-15. 2011
  8. ncbi request reprint Molecular basis of the pharmacological difference between rat and human bombesin receptor subtype-3 (BRS-3)
    Jie Liu
    Department of Obesity and Metabolic Research, Merck Research Laboratories, Rahway, NJ 07065, USA
    Biochemistry 41:8954-60. 2002
  9. ncbi request reprint Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents
    Tung M Fong
    Department of Metabolic Disorders, Merck Research Laboratories, R80M 213, P O Box 2000, Rahway, NJ 07065, USA
    J Pharmacol Exp Ther 321:1013-22. 2007
  10. ncbi request reprint Design and synthesis of (ant)-agonists that alter appetite and adiposity
    Lex H T Van der Ploeg
    Merck Research Laboratories, Boston, MA, USA
    Prog Brain Res 153:107-18. 2006

Collaborators

Detail Information

Publications12

  1. doi request reprint Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist
    Xiao Ming Guan
    Department of Metabolic Disorders, Merck Research Laboratories, Rahway, New Jersey 07065 0900, USA
    J Pharmacol Exp Ther 336:356-64. 2011
    ..Our results demonstrate antiobesity efficacy for MK-5046 in rodents and dogs and further support BRS-3 agonism as a new approach to the treatment of obesity...
  2. doi request reprint Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity
    Jian Liu
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 20:2074-7. 2010
    ..After oral administration, compound 9 had sufficient exposure in diet induced obese mice to demonstrate efficacy in lowering food intake and body weight via BRS-3 activation...
  3. doi request reprint Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity
    Xiao Ming Guan
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Cell Metab 11:101-12. 2010
    ..These results demonstrate that BRS-3 has a role in energy homeostasis that complements several well-known pathways and that BRS-3 agonists represent a potential approach to the treatment of obesity...
  4. doi request reprint Body temperature as a mouse pharmacodynamic response to bombesin receptor subtype-3 agonists and other potential obesity treatments
    Joseph M Metzger
    Departments of Pharmacology, Rahway, NJ 07065, USA
    Am J Physiol Endocrinol Metab 299:E816-24. 2010
    ..The T(b) assay is a robust, information-rich assay that is simpler and has a greater throughput than measuring metabolic rate and is a practical, effective tool for drug discovery...
  5. pmc Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism
    Donald J Marsh
    Department of Obesity Research, Animal Pharmacology, and Comparative Medicine, Merck Research Laboratories, Rahway, NJ 07065, USA
    Proc Natl Acad Sci U S A 99:3240-5. 2002
    ..We conclude that MCH1R is a physiologically relevant MCH receptor in mice that plays a role in energy homeostasis through multiple actions on locomotor activity, metabolism, appetite, and neuroendocrine function...
  6. doi request reprint The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization
    Harry R Chobanian
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem 20:2845-9. 2012
    ..This would thereby make clinical development of this class of compounds more cost effective by inhibiting racemization which can occur over long periods of time at room/elevated temperature...
  7. doi request reprint Bombesin receptor subtype-3 (BRS-3) regulates glucose-stimulated insulin secretion in pancreatic islets across multiple species
    Yue Feng
    Department of Diabetes and Obesity, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Endocrinology 152:4106-15. 2011
    ..Thus, in addition to its potential role in the treatment of obesity, BRS-3 may also regulate blood glucose levels and have a role in the treatment of diabetes mellitus...
  8. ncbi request reprint Molecular basis of the pharmacological difference between rat and human bombesin receptor subtype-3 (BRS-3)
    Jie Liu
    Department of Obesity and Metabolic Research, Merck Research Laboratories, Rahway, NJ 07065, USA
    Biochemistry 41:8954-60. 2002
    ..These results indicate that the sequence variation in the E3 loop is responsible for the species difference between rat and human BRS-3, and multiple residues in the E3 loop are involved in interactions with the agonist dY-bombesin...
  9. ncbi request reprint Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents
    Tung M Fong
    Department of Metabolic Disorders, Merck Research Laboratories, R80M 213, P O Box 2000, Rahway, NJ 07065, USA
    J Pharmacol Exp Ther 321:1013-22. 2007
    ..These studies demonstrated that MK-0364 is a highly potent and selective CB1R inverse agonist and that it is orally active in rodent models of obesity...
  10. ncbi request reprint Design and synthesis of (ant)-agonists that alter appetite and adiposity
    Lex H T Van der Ploeg
    Merck Research Laboratories, Boston, MA, USA
    Prog Brain Res 153:107-18. 2006
    ....
  11. doi request reprint Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists
    Michael M C Lo
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 21:2040-3. 2011
    ..We describe the discovery of 2a, which has mid-nanomolar potency, selectivity for human BRS-3 versus the other bombesin-like receptors, and good bioavailability...
  12. doi request reprint Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists
    Shuwen He
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 20:1913-7. 2010
    ..This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3...