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Page 1
Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists.
Han S, Thoresen L, Zhu X, Narayanan S, Jung JK, Strah-Pleynet S, Decaire M, Choi K, Xiong Y, Yue D, Semple G, Thatte J, Solomon M, Fu L, Whelan K, Al-Shamma H, Gatlin J, Chen R, Dang H, Pride C, Gaidarov I, Unett DJ, Behan DP, Sadeque A, Usmani KA, Chen C, Edwards J, Morgan M, Jones RM. Han S, et al. Among authors: jung jk. Bioorg Med Chem Lett. 2015 Jan 15;25(2):322-6. doi: 10.1016/j.bmcl.2014.11.040. Epub 2014 Nov 26. Bioorg Med Chem Lett. 2015. PMID: 25488844
Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain.
Han S, Thoresen L, Jung JK, Zhu X, Thatte J, Solomon M, Gaidarov I, Unett DJ, Yoon WH, Barden J, Sadeque A, Usmani A, Chen C, Semple G, Grottick AJ, Al-Shamma H, Christopher R, Jones RM. Han S, et al. Among authors: jung jk. ACS Med Chem Lett. 2017 Nov 30;8(12):1309-1313. doi: 10.1021/acsmedchemlett.7b00396. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259753 Free PMC article.
Agonist lead identification for the high affinity niacin receptor GPR109a.
Gharbaoui T, Skinner PJ, Shin YJ, Averbuj C, Jung JK, Johnson BR, Duong T, Decaire M, Uy J, Cherrier MC, Webb PJ, Tamura SY, Zou N, Rodriguez N, Boatman PD, Sage CR, Lindstrom A, Xu J, Schrader TO, Smith BM, Chen R, Richman JG, Connolly DT, Colletti SL, Tata JR, Semple G. Gharbaoui T, et al. Among authors: jung jk. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4914-9. doi: 10.1016/j.bmcl.2007.06.028. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17588745
3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.
Semple G, Skinner PJ, Gharbaoui T, Shin YJ, Jung JK, Cherrier MC, Webb PJ, Tamura SY, Boatman PD, Sage CR, Schrader TO, Chen R, Colletti SL, Tata JR, Waters MG, Cheng K, Taggart AK, Cai TQ, Carballo-Jane E, Behan DP, Connolly DT, Richman JG. Semple G, et al. Among authors: jung jk. J Med Chem. 2008 Aug 28;51(16):5101-8. doi: 10.1021/jm800258p. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665582
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Boatman PD, Schrader TO, Kasem M, Johnson BR, Skinner PJ, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Taggart AK, Carballo-Jane E, Richman JG. Boatman PD, et al. Among authors: jung jk. Bioorg Med Chem Lett. 2010 May 1;20(9):2797-800. doi: 10.1016/j.bmcl.2010.03.062. Epub 2010 Mar 20. Bioorg Med Chem Lett. 2010. PMID: 20363624
(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.
Boatman PD, Lauring B, Schrader TO, Kasem M, Johnson BR, Skinner P, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Luo WL, Caro L, Cote J, Lai E, Wagner J, Taggart AK, Carballo-Jane E, Hammond M, Colletti SL, Tata JR, Connolly DT, Waters MG, Richman JG. Boatman PD, et al. Among authors: jung jk. J Med Chem. 2012 Apr 26;55(8):3644-66. doi: 10.1021/jm2010964. Epub 2012 Apr 9. J Med Chem. 2012. PMID: 22435740 Clinical Trial.
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: jung jk. 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
GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles 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, Taggart AK, Cheng K, Carballo-Jane E, Gerard Waters M, Tata JR, Colletti SL. Imbriglio JE, et al. Among authors: jung jk. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2121-4. doi: 10.1016/j.bmcl.2009.03.014. Epub 2009 Mar 9. Bioorg Med Chem Lett. 2009. PMID: 19307116
388 results