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13 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: haynes ne. J Med Chem. 2012 Aug 23;55(16):7021-36. doi: 10.1021/jm3008689. Epub 2012 Aug 1. J Med Chem. 2012. PMID: 22809456
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: haynes ne. 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. 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: haynes ne. 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.
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: haynes ne. 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
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia.
Kelly MJ, Pietranico-Cole S, Larigan JD, Haynes NE, Reynolds CH, Scott N, Vermeulen J, Dvorozniak M, Conde-Knape K, Huang KS, So SS, Thakkar K, Qian Y, Banner B, Mennona F, Danzi S, Klein I, Taub R, Tilley J. Kelly MJ, et al. Among authors: haynes ne. J Med Chem. 2014 May 22;57(10):3912-23. doi: 10.1021/jm4019299. Epub 2014 Apr 8. J Med Chem. 2014. PMID: 24712661
Identification of an Adamantyl Azaquinolone JNK Selective Inhibitor.
Haynes NE, Scott NR, Chen LC, Janson CA, Li JK, Lukacs CM, Railkar A, Tozzo E, Whittard T, Brown NF, Cheung AW. Haynes NE, et al. ACS Med Chem Lett. 2012 Aug 8;3(9):764-8. doi: 10.1021/ml300175c. eCollection 2012 Sep 13. ACS Med Chem Lett. 2012. PMID: 24900545 Free PMC article.
Metal impurities cause false positives in high-throughput screening campaigns.
Hermann JC, Chen Y, Wartchow C, Menke J, Gao L, Gleason SK, Haynes NE, Scott N, Petersen A, Gabriel S, Vu B, George KM, Narayanan A, Li SH, Qian H, Beatini N, Niu L, Gan QF. Hermann JC, et al. Among authors: haynes ne. ACS Med Chem Lett. 2012 Dec 12;4(2):197-200. doi: 10.1021/ml3003296. eCollection 2013 Feb 14. ACS Med Chem Lett. 2012. PMID: 24900642 Free PMC article.
Multisubstrate analogue based on 5,8,10-trideazafolate.
Boger DL, Haynes NE, Warren MS, Ramcharan J, Kitos PA, Benkovic SJ. Boger DL, et al. Among authors: haynes ne. Bioorg Med Chem. 1997 Sep;5(9):1853-7. doi: 10.1016/s0968-0896(97)00124-7. Bioorg Med Chem. 1997. PMID: 9354241 No abstract available.
13 results