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21 results

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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: guertin kr. 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: guertin kr. 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: guertin kr. 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.
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: guertin kr. Science. 2003 Jul 18;301(5631):370-3. doi: 10.1126/science.1084073. Science. 2003. PMID: 12869762
Discovery of camphor-derived pyrazolones as 11β-hydroxysteroid dehydrogenase type 1 inhibitors.
Gillespie P, Pietranico-Cole S, Myers M, Bilotta JA, Conde-Knape K, Fotouhi N, Goodnow RA Jr, Guertin KR, Hamilton MM, Haynes NE, Liu B, Qi L, Ren Y, Scott NR, So SS, Spence C, Taub R, Thakkar K, Tilley JW, Zwingelstein C. Gillespie P, et al. Among authors: guertin kr. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2707-11. doi: 10.1016/j.bmcl.2014.04.049. Epub 2014 Apr 21. Bioorg Med Chem Lett. 2014. PMID: 24815509
Identification of a novel class of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity.
Guertin KR, Setti L, Qi L, Dunsdon RM, Dymock BW, Jones PS, Overton H, Taylor M, Williams G, Sergi JA, Wang K, Peng Y, Renzetti M, Boyce R, Falcioni F, Garippa R, Olivier AR. Guertin KR, et al. Bioorg Med Chem Lett. 2003 Sep 1;13(17):2895-8. doi: 10.1016/s0960-894x(03)00623-1. Bioorg Med Chem Lett. 2003. PMID: 14611852
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.
Guertin KR, Gardner CJ, Klein SI, Zulli AL, Czekaj M, Gong Y, Spada AP, Cheney DL, Maignan S, Guilloteau JP, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Dunwiddie CT, Leadley RJ, Pauls HW. Guertin KR, et al. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1671-4. doi: 10.1016/s0960-894x(02)00213-5. Bioorg Med Chem Lett. 2002. PMID: 12039587
21 results