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Page 1
Novel glucokinase activators: a patent review (2008 - 2010).
Sarabu R, Berthel SJ, Kester RF, Tilley JW. Sarabu R, et al. Among authors: kester rf. Expert Opin Ther Pat. 2011 Jan;21(1):13-33. doi: 10.1517/13543776.2011.542413. Epub 2010 Dec 15. Expert Opin Ther Pat. 2011. PMID: 21155690 Review.
Allosteric activators of glucokinase: potential role in diabetes therapy.
Grimsby J, Sarabu R, Corbett WL, Haynes NE, Bizzarro FT, Coffey JW, Guertin KR, Hilliard DW, Kester RF, Mahaney PE, Marcus L, Qi L, Spence CL, Tengi J, Magnuson MA, Chu CA, Dvorozniak MT, Matschinsky FM, Grippo JF. Grimsby J, et al. Among authors: kester rf. Science. 2003 Jul 18;301(5631):370-3. doi: 10.1126/science.1084073. Science. 2003. PMID: 12869762
2,3-Disubstituted acrylamides as potent glucokinase activators.
Sidduri A, Grimsby JS, Corbett WL, Sarabu R, Grippo JF, Lou J, Kester RF, Dvorozniak M, Marcus L, Spence C, Racha JK, Moore DJ. Sidduri A, et al. Among authors: kester rf. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5673-6. doi: 10.1016/j.bmcl.2010.08.029. Epub 2010 Aug 11. Bioorg Med Chem Lett. 2010. PMID: 20805029
Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
Sarabu R, Bizzarro FT, Corbett WL, Dvorozniak MT, Geng W, Grippo JF, Haynes NE, Hutchings S, Garofalo L, Guertin KR, Hilliard DW, Kabat M, Kester RF, Ka W, Liang Z, Mahaney PE, Marcus L, Matschinsky FM, Moore D, Racha J, Radinov R, Ren Y, Qi L, Pignatello M, Spence CL, Steele T, Tengi J, Grimsby J. Sarabu R, et al. Among authors: kester rf. J Med Chem. 2012 Aug 23;55(16):7021-36. doi: 10.1021/jm3008689. Epub 2012 Aug 1. J Med Chem. 2012. PMID: 22809456
Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide (RO0281675).
Haynes NE, Corbett WL, Bizzarro FT, Guertin KR, Hilliard DW, Holland GW, Kester RF, Mahaney PE, Qi L, Spence CL, Tengi J, Dvorozniak MT, Railkar A, Matschinsky FM, Grippo JF, Grimsby J, Sarabu R. Haynes NE, et al. Among authors: kester rf. J Med Chem. 2010 May 13;53(9):3618-25. doi: 10.1021/jm100039a. J Med Chem. 2010. PMID: 20405948
Identification of RO4597014, a Glucokinase Activator Studied in the Clinic for the Treatment of Type 2 Diabetes.
Qian Y, Corbett WL, Berthel SJ, Choi DS, Dvorozniak MT, Geng W, Gillespie P, Guertin KR, Haynes NE, Kester RF, Mennona FA, Moore D, Racha J, Radinov R, Sarabu R, Scott NR, Grimsby J, Mallalieu NL. Qian Y, et al. Among authors: kester rf. ACS Med Chem Lett. 2013 Mar 7;4(4):414-8. doi: 10.1021/ml400027y. eCollection 2013 Apr 11. ACS Med Chem Lett. 2013. PMID: 24900686 Free PMC article.
Potent, selective MCH-1 receptor antagonists.
Erickson SD, Banner B, Berthel S, Conde-Knape K, Falcioni F, Hakimi I, Hennessy B, Kester RF, Kim K, Ma C, McComas W, Mennona F, Mischke S, Orzechowski L, Qian Y, Salari H, Tengi J, Thakkar K, Taub R, Tilley JW, Wang H. Erickson SD, et al. Among authors: kester rf. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1402-6. doi: 10.1016/j.bmcl.2008.01.010. Epub 2008 Jan 8. Bioorg Med Chem Lett. 2008. PMID: 18243691
Optimization of benzodiazepinones as selective inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) second baculovirus IAP repeat (BIR2) domain.
Kester RF, Donnell AF, Lou Y, Remiszewski SW, Lombardo LJ, Chen S, Le NT, Lo J, Moliterni JA, Han X, Hogg JH, Liang W, Michoud C, Rupert KC, Mischke S, Le K, Weisel M, Janson CA, Lukacs CM, Fretland AJ, Hong K, Polonskaia A, Gao L, Li S, Solis DS, Aguilar D, Tardell C, Dvorozniak M, Tannu S, Lee EC, Schutt AD, Goggin B. Kester RF, et al. J Med Chem. 2013 Oct 24;56(20):7788-803. doi: 10.1021/jm400732v. Epub 2013 Oct 7. J Med Chem. 2013. PMID: 24093940
Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus IAP repeat (BIR2) domain.
Donnell AF, Michoud C, Rupert KC, Han X, Aguilar D, Frank KB, Fretland AJ, Gao L, Goggin B, Hogg JH, Hong K, Janson CA, Kester RF, Kong N, Le K, Li S, Liang W, Lombardo LJ, Lou Y, Lukacs CM, Mischke S, Moliterni JA, Polonskaia A, Schutt AD, Solis DS, Specian A, Taylor RT, Weisel M, Remiszewski SW. Donnell AF, et al. Among authors: kester rf. J Med Chem. 2013 Oct 24;56(20):7772-87. doi: 10.1021/jm400731m. Epub 2013 Oct 1. J Med Chem. 2013. PMID: 24083782