Lafontaine JA - Search Results

1

Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.

Lafontaine JA, Day RF, Dibrino J, Hadcock JR, Hargrove DM, Linhares M, Martin KA, Maurer TS, Nardone NA, Tess DA, Dasilva-Jardine P. Lafontaine JA, et al. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5245-50. doi: 10.1016/j.bmcl.2007.06.072. Epub 2007 Jun 30. Bioorg Med Chem Lett. 2007. PMID: 17632003

2

Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.

Humphries PS, Lafontaine JA, Agree CS, Alexander D, Chen P, Do QQ, Li LY, Lunney EA, Rajapakse RJ, Siegel K, Timofeevski SL, Wang T, Wilhite DM. Humphries PS, et al. Among authors: lafontaine ja. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2099-102. doi: 10.1016/j.bmcl.2009.03.023. Epub 2009 Mar 13. Bioorg Med Chem Lett. 2009. PMID: 19327989

3

Identification of novel pyrrolopyrazoles as protein kinase C β II inhibitors.

Li H, Hong Y, Nukui S, Lou J, Johnson S, Scales S, Botrous I, Tompkins E, Yin C, Zhou R, He M, Jensen J, Bouzida D, Alton G, Lafontaine J, Grant S. Li H, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):584-7. doi: 10.1016/j.bmcl.2010.10.032. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2011. PMID: 21084194

4

Discovery of a novel class of targeted kinase inhibitors that blocks protein kinase C signaling and ameliorates retinal vascular leakage in a diabetic rat model.

Grant S, Tran P, Zhang Q, Zou A, Dinh D, Jensen J, Zhou S, Kang X, Zachwieja J, Lippincott J, Liu K, Johnson SL, Scales S, Yin C, Nukui S, Stoner C, Prasanna G, Lafontaine J, Wells P, Li H. Grant S, et al. Eur J Pharmacol. 2010 Feb 10;627(1-3):16-25. doi: 10.1016/j.ejphar.2009.10.029. Epub 2009 Oct 20. Eur J Pharmacol. 2010. PMID: 19850035

5

Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.

Prasanna G, Carreiro S, Anderson S, Gukasyan H, Sartnurak S, Younis H, Gale D, Xiang C, Wells P, Dinh D, Almaden C, Fortner J, Toris C, Niesman M, Lafontaine J, Krauss A. Prasanna G, et al. Exp Eye Res. 2011 Sep;93(3):256-64. doi: 10.1016/j.exer.2011.02.015. Epub 2011 Mar 3. Exp Eye Res. 2011. PMID: 21376717

6

Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure.

Huang Q, Rui EY, Cobbs M, Dinh DM, Gukasyan HJ, Lafontaine JA, Mehta S, Patterson BD, Rewolinski DA, Richardson PF, Edwards MP. Huang Q, et al. Among authors: lafontaine ja. J Med Chem. 2015 Mar 26;58(6):2821-33. doi: 10.1021/acs.jmedchem.5b00043. Epub 2015 Mar 6. J Med Chem. 2015. PMID: 25728019

7

Ocular pharmacokinetics and hypotensive activity of PF-04475270, an EP4 prostaglandin agonist in preclinical models.

Prasanna G, Fortner J, Xiang C, Zhang E, Carreiro S, Anderson S, Sartnurak S, Wu G, Gukasyan H, Niesman M, Nair S, Rui E, Lafontaine J, Almaden CD, Wells P, Krauss A. Prasanna G, et al. Exp Eye Res. 2009 Nov;89(5):608-17. doi: 10.1016/j.exer.2009.05.002. Epub 2009 May 13. Exp Eye Res. 2009. PMID: 19445930

8

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.

Cheng H, Nair SK, Murray BW, Almaden C, Bailey S, Baxi S, Behenna D, Cho-Schultz S, Dalvie D, Dinh DM, Edwards MP, Feng JL, Ferre RA, Gajiwala KS, Hemkens MD, Jackson-Fisher A, Jalaie M, Johnson TO, Kania RS, Kephart S, Lafontaine J, Lunney B, Liu KK, Liu Z, Matthews J, Nagata A, Niessen S, Ornelas MA, Orr ST, Pairish M, Planken S, Ren S, Richter D, Ryan K, Sach N, Shen H, Smeal T, Solowiej J, Sutton S, Tran K, Tseng E, Vernier W, Walls M, Wang S, Weinrich SL, Xin S, Xu H, Yin MJ, Zientek M, Zhou R, Kath JC. Cheng H, et al. J Med Chem. 2016 Mar 10;59(5):2005-24. doi: 10.1021/acs.jmedchem.5b01633. Epub 2016 Jan 28. J Med Chem. 2016. PMID: 26756222

9

Discovery of Highly Selective Inhibitors of Microtubule-Associated Serine/Threonine Kinase-like (MASTL).

Gallego RA, Scales S, Toledo C, Auth M, Bernier L, Berry M, Brun S, Chung L, Davis C, Diehl W, Dress K, Eisele K, Elleraas J, Ewanicki J, Fobian Y, Greasley S, Greenwald EC, Johnson TW, Khamphavong P, Lafontaine J, Li J, Linton A, Maestre M, Miller N, Murtaza A, Patman RL, Quinlan CL, Ramms DJ, Richardson P, Sach N, Salomon-Ferrer R, Silva F, Timofeevski S, Tran P, Tran-Dubé M, Wang F, Wang W, Wythes M, Yang S, Zou A, VanArsdale T, McAlpine I. Gallego RA, et al. J Med Chem. 2024 Nov 14;67(21):19234-19246. doi: 10.1021/acs.jmedchem.4c01659. Epub 2024 Nov 5. J Med Chem. 2024. PMID: 39499084

10

Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.

Planken S, Behenna DC, Nair SK, Johnson TO, Nagata A, Almaden C, Bailey S, Ballard TE, Bernier L, Cheng H, Cho-Schultz S, Dalvie D, Deal JG, Dinh DM, Edwards MP, Ferre RA, Gajiwala KS, Hemkens M, Kania RS, Kath JC, Matthews J, Murray BW, Niessen S, Orr ST, Pairish M, Sach NW, Shen H, Shi M, Solowiej J, Tran K, Tseng E, Vicini P, Wang Y, Weinrich SL, Zhou R, Zientek M, Liu L, Luo Y, Xin S, Zhang C, Lafontaine J. Planken S, et al. J Med Chem. 2017 Apr 13;60(7):3002-3019. doi: 10.1021/acs.jmedchem.6b01894. Epub 2017 Mar 29. J Med Chem. 2017. PMID: 28287730

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