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249 results

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Page 1
Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality.
Liu P, Lanza TJ Jr, Chioda M, Jones C, Chobanian HR, Guo Y, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM, Marsh DJ, Metzger JM, Ramsay K, Wang SP, Strack AM, Miller R, Pang J, Lyons K, Dragovic J, Ning JG, Schafer WA, Welch CJ, Gong X, Gao YD, Hornak V, Ball RG, Tsou N, Reitman ML, Wyvratt MJ, Nargund RP, Lin LS. Liu P, et al. Among authors: metzger jm. ACS Med Chem Lett. 2011 Oct 3;2(12):933-7. doi: 10.1021/ml200207w. eCollection 2011 Dec 8. ACS Med Chem Lett. 2011. PMID: 24900283 Free PMC article.
Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.
He S, Dobbelaar PH, Liu J, Jian T, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M, Henderson AJ, Ruenz M, Sargent BJ, Yet L, Kelly TM, Palyha O, Kan Y, Pan J, Chen H, Marsh DJ, Shearman LP, Strack AM, Metzger JM, Feighner SD, Tan C, Howard AD, Tamvakopoulos C, Peng Q, Guan XM, Reitman ML, Patchett AA, Wyvratt MJ Jr, Nargund RP. He S, et al. Among authors: metzger jm. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1913-7. doi: 10.1016/j.bmcl.2010.01.154. Epub 2010 Feb 4. Bioorg Med Chem Lett. 2010. PMID: 20167483
Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
Liu J, He S, Jian T, Dobbelaar PH, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M, Henderson AJ, Pattamana K, Ruenz M, Sargent BJ, Swenson B, Yet L, Tamvakopoulos C, Peng Q, Pan J, Kan Y, Palyha O, Kelly TM, Guan XM, Howard AD, Marsh DJ, Metzger JM, Reitman ML, Wyvratt MJ, Nargund RP. Liu J, et al. Among authors: metzger jm. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2074-7. doi: 10.1016/j.bmcl.2010.02.076. Epub 2010 Feb 21. Bioorg Med Chem Lett. 2010. PMID: 20219372
Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist.
Guan XM, Metzger JM, Yang L, Raustad KA, Wang SP, Spann SK, Kosinski JA, Yu H, Shearman LP, Faidley TD, Palyha O, Kan Y, Kelly TM, Sebhat I, Lin LS, Dragovic J, Lyons KA, Craw S, Nargund RP, Marsh DJ, Strack AM, Reitman ML. Guan XM, et al. Among authors: metzger jm. J Pharmacol Exp Ther. 2011 Feb;336(2):356-64. doi: 10.1124/jpet.110.174763. Epub 2010 Oct 29. J Pharmacol Exp Ther. 2011. PMID: 21036912
The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization.
Chobanian HR, Guo Y, Liu P, Lanza TJ Jr, Chioda M, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM, Marsh DJ, Metzger JM, Raustad K, Wang SP, Strack AM, Gorski JN, Miller R, Pang J, Lyons K, Dragovic J, Ning JG, Schafer WA, Welch CJ, Gong X, Gao YD, Hornak V, Reitman ML, Nargund RP, Lin LS. Chobanian HR, et al. Among authors: metzger jm. Bioorg Med Chem. 2012 May 1;20(9):2845-9. doi: 10.1016/j.bmc.2012.03.029. Epub 2012 Mar 24. Bioorg Med Chem. 2012. PMID: 22494842
Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Sebhat IK, Franklin C, Lo MM, Chen D, Jewell JP, Miller R, Pang J, Palyha O, Kan Y, Kelly TM, Guan XM, Marsh DJ, Kosinski JA, Metzger JM, Lyons K, Dragovic J, Guzzo PR, Henderson AJ, Reitman ML, Nargund RP, Wyvratt MJ, Lin LS. Sebhat IK, et al. Among authors: metzger jm. ACS Med Chem Lett. 2010 Oct 18;2(1):43-7. doi: 10.1021/ml100196d. eCollection 2011 Jan 13. ACS Med Chem Lett. 2010. PMID: 24900253 Free PMC article.
Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Chobanian HR, Guo Y, Liu P, Chioda M, Lanza TJ Jr, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM, Marsh DJ, Metzger JM, Gorski JN, Raustad K, Wang SP, Strack AM, Miller R, Pang J, Madeira M, Lyons K, Dragovic J, Reitman ML, Nargund RP, Lin LS. Chobanian HR, et al. Among authors: metzger jm. ACS Med Chem Lett. 2012 Jan 21;3(3):252-6. doi: 10.1021/ml200304j. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900461 Free PMC article.
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA. Palucki BL, et al. Among authors: metzger jm. Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5. doi: 10.1016/j.bmcl.2004.10.020. Bioorg Med Chem Lett. 2005. PMID: 15582434
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Ye Z, Guo L, Barakat KJ, Pollard PG, Palucki BL, Sebhat IK, Bakshi RK, Tang R, Kalyani RN, Vongs A, Chen AS, Chen HY, Rosenblum CI, MacNeil T, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen DE, Martin WJ, Metzger JM, Strack AM, MacIntyre DE, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP. Ye Z, et al. Among authors: metzger jm. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5. doi: 10.1016/j.bmcl.2005.05.109. Bioorg Med Chem Lett. 2005. PMID: 15982875
Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Guan XM, Chen H, Dobbelaar PH, Dong Y, Fong TM, Gagen K, Gorski J, He S, Howard AD, Jian T, Jiang M, Kan Y, Kelly TM, Kosinski J, Lin LS, Liu J, Marsh DJ, Metzger JM, Miller R, Nargund RP, Palyha O, Shearman L, Shen Z, Stearns R, Strack AM, Stribling S, Tang YS, Wang SP, White A, Yu H, Reitman ML. Guan XM, et al. Among authors: metzger jm. Cell Metab. 2010 Feb 3;11(2):101-12. doi: 10.1016/j.cmet.2009.12.008. Epub 2010 Jan 21. Cell Metab. 2010. PMID: 20096642 Free article.
249 results