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Items: 13

1.

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.

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2707-11. doi: 10.1016/j.bmcl.2014.04.049. Epub 2014 Apr 21.

PMID:
24815509
2.

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.

ACS Med Chem Lett. 2013 Mar 7;4(4):414-8. doi: 10.1021/ml400027y. eCollection 2013 Apr 11.

3.

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.

J Med Chem. 2012 Aug 23;55(16):7021-36. doi: 10.1021/jm3008689. Epub 2012 Aug 1.

PMID:
22809456
4.

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.

J Med Chem. 2010 May 13;53(9):3618-25. doi: 10.1021/jm100039a.

PMID:
20405948
5.

The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development.

Guertin KR, Choi YM.

Curr Med Chem. 2007;14(23):2471-81. Review.

PMID:
17979700
6.

Small molecule glucokinase activators as glucose lowering agents: a new paradigm for diabetes therapy.

Guertin KR, Grimsby J.

Curr Med Chem. 2006;13(15):1839-43. Review.

PMID:
16787225
7.

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.

Bioorg Med Chem Lett. 2003 Sep 1;13(17):2895-8.

PMID:
14611852
8.

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.

Science. 2003 Jul 18;301(5631):370-3.

9.

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.

Bioorg Med Chem Lett. 2002 Jun 17;12(12):1671-4.

PMID:
12039587
10.

Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.

Czekaj M, Klein SI, Guertin KR, Gardner CJ, Zulli AL, Pauls HW, Spada AP, Cheney DL, Brown KD, Colussi DJ, Chu V, Leadley RJ, Dunwiddie CT.

Bioorg Med Chem Lett. 2002 Jun 17;12(12):1667-70.

PMID:
12039586
11.

Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa.

Klein SI, Czekaj M, Gardner CJ, Guertin KR, Cheney DL, Spada AP, Bolton SA, Brown K, Colussi D, Heran CL, Morgan SR, Leadley RJ, Dunwiddie CT, Perrone MH, Chu V.

J Med Chem. 1998 Feb 12;41(4):437-50.

PMID:
9484495
12.

Functional analysis of the Pseudomonas aeruginosa autoinducer PAI.

Passador L, Tucker KD, Guertin KR, Journet MP, Kende AS, Iglewski BH.

J Bacteriol. 1996 Oct;178(20):5995-6000.

13.

Bilateral acetylsulfapyridine nephrolithiasis associated with chronic sulfasalazine therapy.

Erturk E, Casemento JB, Guertin KR, Kende AS.

J Urol. 1994 Jun;151(6):1605-6.

PMID:
7910643

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