Philippe Bergeron

发表

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

C. Ly, S. Sideris, S. Malek, 2011, Journal of medicinal chemistry.

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

C. Ly, S. Sideris, S. Malek, 2012, Journal of medicinal chemistry.

Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.

Brian J. Smith, J. Baell, G. Nikolakopoulos, 2014, ACS medicinal chemistry letters.

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.

S. Sideris, S. Malek, J. Lyssikatos, 2013, Bioorganic & medicinal chemistry letters.

Access to Saturated Fused PyrimidineDerivatives via a Flexible N-Vinyl TertiaryEnamide Synthesis

J. Lyssikatos, Anthony A. Estrada, Philippe Bergeron, 2011 .

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.

K. Bowman, Jiansheng Wu, R. Firestein, 2016, ACS medicinal chemistry letters.

Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.

C. Ly, W. Fairbrother, V. Tsui, 2010, Bioorganic & medicinal chemistry letters.

Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations.

Adam R. Johnson, C. Eigenbrot, A. Estevez, 2016, ACS chemical biology.

Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.

Jane R Kenny, Philippe Bergeron, Ignacio Aliagas, 2013, Journal of medicinal chemistry.

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.

Jane R Kenny, Philippe Bergeron, Tian Jin, 2012, Journal of medicinal chemistry.

Cryo-EM reveals an unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors

M. Volgraf, A. Rohou, C. Arthur, 2022, bioRxiv.

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain.

D. Sutherlin, Jun Chen, D. Hackos, 2019, Journal of medicinal chemistry.

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.

Philippe Bergeron, Kevin R Clark, James R Kiefer, 2016, ACS medicinal chemistry letters.

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

M. Belvin, C. Ly, S. Sideris, 2013, ACS medicinal chemistry letters.

Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.

Jane R Kenny, Philippe Bergeron, Charles Eigenbrot, 2012, Bioorganic & medicinal chemistry letters.

Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310.

D. Sutherlin, Jun Chen, D. Hackos, 2021, Journal of medicinal chemistry.

An integrated suite of modeling tools that empower scientists in structure- and property-based drug design

Jeffrey M. Blaney, Philippe Bergeron, Man-Ling Lee, 2015, Journal of Computer-Aided Molecular Design.

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.

K. Bowman, Jiansheng Wu, R. Firestein, 2016, ACS medicinal chemistry letters.

Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.

Adam R. Johnson, Rohan V Mendonca, M. Ultsch, 2012, Bioorganic & medicinal chemistry letters.