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Page 1
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).
Fotsch C, Smith DM, Adams JA, Cheetham J, Croghan M, Doherty EM, Hale C, Jarosinski MA, Kelly MG, Norman MH, Tamayo NA, Xi N, Baumgartner JW. Fotsch C, et al. Among authors: norman mh. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2337-40. doi: 10.1016/s0960-894x(03)00412-8. Bioorg Med Chem Lett. 2003. PMID: 12824029
AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties.
Gavva NR, Tamir R, Qu Y, Klionsky L, Zhang TJ, Immke D, Wang J, Zhu D, Vanderah TW, Porreca F, Doherty EM, Norman MH, Wild KD, Bannon AW, Louis JC, Treanor JJ. Gavva NR, et al. Among authors: norman mh. J Pharmacol Exp Ther. 2005 Apr;313(1):474-84. doi: 10.1124/jpet.104.079855. Epub 2004 Dec 22. J Pharmacol Exp Ther. 2005. PMID: 15615864
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Fotsch C, Han N, Arasasingham P, Bo Y, Carmouche M, Chen N, Davis J, Goldberg MH, Hale C, Hsieh FY, Kelly MG, Liu Q, Norman MH, Smith DM, Stec M, Tamayo N, Xi N, Xu S, Bannon AW, Baumgartner JW. Fotsch C, et al. Among authors: norman mh. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1623-7. doi: 10.1016/j.bmcl.2005.01.060. Bioorg Med Chem Lett. 2005. PMID: 15745810
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.
Ognyanov VI, Balan C, Bannon AW, Bo Y, Dominguez C, Fotsch C, Gore VK, Klionsky L, Ma VV, Qian YX, Tamir R, Wang X, Xi N, Xu S, Zhu D, Gavva NR, Treanor JJ, Norman MH. Ognyanov VI, et al. Among authors: norman mh. J Med Chem. 2006 Jun 15;49(12):3719-42. doi: 10.1021/jm060065y. J Med Chem. 2006. PMID: 16759115
The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation.
Gavva NR, Bannon AW, Surapaneni S, Hovland DN Jr, Lehto SG, Gore A, Juan T, Deng H, Han B, Klionsky L, Kuang R, Le A, Tamir R, Wang J, Youngblood B, Zhu D, Norman MH, Magal E, Treanor JJ, Louis JC. Gavva NR, et al. Among authors: norman mh. J Neurosci. 2007 Mar 28;27(13):3366-74. doi: 10.1523/JNEUROSCI.4833-06.2007. J Neurosci. 2007. PMID: 17392452 Free PMC article.
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Biswas K, Li A, Chen JJ, D'Amico DC, Fotsch C, Han N, Human J, Liu Q, Norman MH, Riahi B, Yuan C, Suzuki H, Mareska DA, Zhan J, Clarke DE, Toro A, Groneberg RD, Burgess LE, Lester-Zeiner D, Biddlecome G, Manning BH, Arik L, Dong H, Huang M, Kamassah A, Loeloff R, Sun H, Hsieh FY, Kumar G, Ng GY, Hungate RW, Askew BC, Johnson E. Biswas K, et al. Among authors: norman mh. J Med Chem. 2007 May 3;50(9):2200-12. doi: 10.1021/jm070055c. Epub 2007 Apr 5. J Med Chem. 2007. PMID: 17408249
71 results