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Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Shen HC, Ding FX, Raghavan S, Deng Q, Luell S, Forrest MJ, Carballo-Jane E, Wilsie LC, Krsmanovic ML, Taggart AK, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: holt tg. J Med Chem. 2010 Mar 25;53(6):2666-70. doi: 10.1021/jm100022r. J Med Chem. 2010. PMID: 20184326
Discovery of imidazole carboxamides as potent and selective CCK1R agonists.
Zhu C, Hansen AR, Bateman T, Chen Z, Holt TG, Hubert JA, Karanam BV, Lee SJ, Pan J, Qian S, Reddy VB, Reitman ML, Strack AM, Tong V, Weingarth DT, Wolff MS, MacNeil DJ, Weber AE, Duffy JL, Edmondson SD. Zhu C, et al. Among authors: holt tg. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4393-6. doi: 10.1016/j.bmcl.2008.06.057. Epub 2008 Jun 20. Bioorg Med Chem Lett. 2008. PMID: 18614364
GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.
Imbriglio JE, Chang S, Liang R, Raghavan S, Schmidt D, Smenton A, Tria S, Schrader TO, Jung JK, Esser C, Holt TG, Wolff MS, Taggart AK, Cheng K, Carballo-Jane E, Waters MG, Tata JR, Colletti SL. Imbriglio JE, et al. Among authors: holt tg. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4472-4. doi: 10.1016/j.bmcl.2010.06.041. Epub 2010 Jun 10. Bioorg Med Chem Lett. 2010. PMID: 20615702
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Shen HC, Ding FX, Deng Q, Wilsie LC, Krsmanovic ML, Taggart AK, Carballo-Jane E, Ren N, Cai TQ, Wu TJ, Wu KK, Cheng K, Chen Q, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: holt tg. J Med Chem. 2009 Apr 23;52(8):2587-602. doi: 10.1021/jm900151e. J Med Chem. 2009. PMID: 19309152
Anthranilic acid replacements in a niacin receptor agonist.
Schmidt D, Smenton A, Raghavan S, Shen H, Ding FX, Carballo-Jane E, Luell S, Ciecko T, Holt TG, Wolff M, Taggart A, Wilsie L, Krsmanovic M, Ren N, Blom D, Cheng K, McCann PE, Waters MG, Tata J, Colletti S. Schmidt D, et al. Among authors: holt tg. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3426-30. doi: 10.1016/j.bmcl.2010.04.001. Epub 2010 Apr 8. Bioorg Med Chem Lett. 2010. PMID: 20444602
22 results