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Page 1
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: corbett wl. J Med Chem. 2010 May 13;53(9):3618-25. doi: 10.1021/jm100039a. J Med Chem. 2010. PMID: 20405948
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: corbett wl. 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: corbett wl. 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: corbett wl. J Med Chem. 2012 Aug 23;55(16):7021-36. doi: 10.1021/jm3008689. Epub 2012 Aug 1. J Med Chem. 2012. PMID: 22809456
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: corbett wl. 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.