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Page 1
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: grimsby j. J Med Chem. 2012 Aug 23;55(16):7021-36. doi: 10.1021/jm3008689. Epub 2012 Aug 1. J Med Chem. 2012. PMID: 22809456
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: grimsby js. 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
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. Science. 2003 Jul 18;301(5631):370-3. doi: 10.1126/science.1084073. Science. 2003. PMID: 12869762
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: grimsby j. 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: grimsby j. 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.
Piragliatin (RO4389620), a novel glucokinase activator, lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus: a mechanistic study.
Bonadonna RC, Heise T, Arbet-Engels C, Kapitza C, Avogaro A, Grimsby J, Zhi J, Grippo JF, Balena R. Bonadonna RC, et al. Among authors: grimsby j. J Clin Endocrinol Metab. 2010 Nov;95(11):5028-36. doi: 10.1210/jc.2010-1041. Epub 2010 Aug 25. J Clin Endocrinol Metab. 2010. PMID: 20739378 Clinical Trial.
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.
Cheung AW, Brinkman J, Firooznia F, Flohr A, Grimsby J, Gubler ML, Guertin K, Hamid R, Marcopulos N, Norcross RD, Qi L, Ramsey G, Tan J, Wen Y, Sarabu R. Cheung AW, et al. Among authors: grimsby j. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4140-6. doi: 10.1016/j.bmcl.2010.05.056. Epub 2010 May 20. Bioorg Med Chem Lett. 2010. PMID: 20541935
115 results