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Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.
Cheng H, Li C, Bailey S, Baxi SM, Goulet L, Guo L, Hoffman J, Jiang Y, Johnson TO, Johnson TW, Knighton DR, Li J, Liu KK, Liu Z, Marx MA, Walls M, Wells PA, Yin MJ, Zhu J, Zientek M. Cheng H, et al. Among authors: goulet l. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7. doi: 10.1021/ml300309h. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900568 Free PMC article.
Identification of novel HSP90α/β isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as Huntington's disease.
Ernst JT, Neubert T, Liu M, Sperry S, Zuccola H, Turnbull A, Fleck B, Kargo W, Woody L, Chiang P, Tran D, Chen W, Snyder P, Alcacio T, Nezami A, Reynolds J, Alvi K, Goulet L, Stamos D. Ernst JT, et al. Among authors: goulet l. J Med Chem. 2014 Apr 24;57(8):3382-400. doi: 10.1021/jm500042s. Epub 2014 Apr 10. J Med Chem. 2014. PMID: 24673104
Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2).
Rowbottom MW, Bain G, Calderon I, Lasof T, Lonergan D, Lai A, Huang F, Darlington J, Prodanovich P, Santini AM, King CD, Goulet L, Shannon KE, Ma GL, Nguyen K, MacKenna DA, Evans JF, Hutchinson JH. Rowbottom MW, et al. Among authors: goulet l. J Med Chem. 2017 May 25;60(10):4403-4423. doi: 10.1021/acs.jmedchem.7b00345. Epub 2017 May 15. J Med Chem. 2017. PMID: 28471663
Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism.
Zhao J, Wang S, Hee Kim S, Han S, Rico-Bautista E, Sturchler E, Nguyen J, Tan H, Staley C, Karin Kusnetzow A, Betz SF, Johns M, Goulet L, Luo R, Fowler M, Athanacio J, Markison S, Scott Struthers R, Zhu Y. Zhao J, et al. Among authors: goulet l. Bioorg Med Chem Lett. 2022 Sep 1;71:128807. doi: 10.1016/j.bmcl.2022.128807. Epub 2022 May 20. Bioorg Med Chem Lett. 2022. PMID: 35605837
Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis.
Bain G, Shannon KE, Huang F, Darlington J, Goulet L, Prodanovich P, Ma GL, Santini AM, Stein AJ, Lonergan D, King CD, Calderon I, Lai A, Hutchinson JH, Evans JF. Bain G, et al. Among authors: goulet l. J Pharmacol Exp Ther. 2017 Jan;360(1):1-13. doi: 10.1124/jpet.116.237156. Epub 2016 Oct 17. J Pharmacol Exp Ther. 2017. PMID: 27754931
Autotaxin activity increases locally following lung injury, but is not required for pulmonary lysophosphatidic acid production or fibrosis.
Black KE, Berdyshev E, Bain G, Castelino FV, Shea BS, Probst CK, Fontaine BA, Bronova I, Goulet L, Lagares D, Ahluwalia N, Knipe RS, Natarajan V, Tager AM. Black KE, et al. Among authors: goulet l. FASEB J. 2016 Jun;30(6):2435-50. doi: 10.1096/fj.201500197R. Epub 2016 Mar 22. FASEB J. 2016. PMID: 27006447 Free PMC article.
., Shea, B. S., Probst, C. K., Fontaine, B. A., Bronova, I., Goulet, L., Lagares, D., Ahluwalia, N., Knipe, R. S., Natarajan, V., Tager, A. ...
., Shea, B. S., Probst, C. K., Fontaine, B. A., Bronova, I., Goulet, L., Lagares, D., Ahluwalia, N., Knipe, R. S., Natarajan, …
97 results