Research Topics
Genomes and Genes | Xiao Ming GuanSummaryAffiliation: GlaxoSmithKline Research and Development Country: USA Publications
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Detail Information
Publications
Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonistXiao 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...- Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesityJian 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... - Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesityXiao 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... - Body temperature as a mouse pharmacodynamic response to bombesin receptor subtype-3 agonists and other potential obesity treatmentsJoseph 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... 
Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolismDonald 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...- The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerizationHarry 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... - Bombesin receptor subtype-3 (BRS-3) regulates glucose-stimulated insulin secretion in pancreatic islets across multiple speciesYue 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... 
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...- 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 rodentsTung 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... - Design and synthesis of (ant)-agonists that alter appetite and adiposityLex H T Van der Ploeg
Merck Research Laboratories, Boston, MA, USA
Prog Brain Res 153:107-18. 2006.... - Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonistsMichael 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... - Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonistsShuwen 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...