Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Fell Jay Bradford"'
Autor:
Joshua Ballard, Harrah Chiang, James G. Christensen, Kenneth Hee, Tony Pisal Tang, Brian R. Baer, Peter Olson, Henry J. Zecca, David Briere, Mark Joseph Chicarelli, Laurence E. Burgess, Karyn Bouhana, Jill Hallin, Matthew A. Marx, Lauren Hanson, Barbara J. Brandhuber, Michael Burkard, Fell Jay Bradford, Pavel Savechenkov, James F. Blake, John P. Fischer, Guy Vigers, Hicken Erik James, Niranjan Sudhakar, Kevin Davidson, Ronald Jay Hinklin, Macedonio J. Mejia, John Gaudino
Publikováno v:
ACS Medicinal Chemistry Letters. 9:1230-1234
[Image: see text] KRAS is the most frequently mutated driver oncogene in human cancer, and KRAS mutations are commonly associated with poor prognosis and resistance to standard treatment. The ability to effectively target and block the function of mu
Autor:
James G. Christensen, Macedonia J. Mejia, Tony Pisal Tang, Joshua Ballard, Pavel Y. Savechenkov, Mark Joseph Chicarelli, Guy Vigers, Niranjan Sudhakar, James F. Blake, Peter D. Olson, Brian R. Baer, David Briere, Matthew A. Marx, Fell Jay Bradford, Michael R. Burkhard, Karyn Bouhana, Laurence E. Burgess, Jill Hallin, Harrah Chiang, John P. Fischer
Publikováno v:
Molecular Cancer Research. 18:B30-B30
The ability to effectively target mutated KRAS has remained elusive despite decades of research. By solving a highly informative set of ligand-complexed co-crystal structures coupled with iterative structure-based drug design, substituted tetrahydrop
Autor:
David Briere, Lauren Hargis, James G. Christensen, Matthew A. Marx, Jill Hallin, Fell Jay Bradford, Lars D. Engstrom, Niranjan Sudhakar, Peter D. Olson, Andrew Calinisan, Michael R. Burkhard, John P. Fischer, Harrah Chiang, Ruth Aranda, Brian R. Baer
Publikováno v:
Molecular Cancer Research. 18:B23-B23
KRAS G12C is a driver mutation and the most frequent KRAS mutation in lung cancer. The ability to effectively target mutated KRAS has remained elusive despite decades of research. A structure-based drug design discovery program identified mutant-sele
Autor:
Peter Olson, David Briere, Matthew A. Marx, Andrew Calinisan, Michael R. Burkhard, Niranjan Sudhakar, Jill Hallin, Lauren Hargis, Fell Jay Bradford, Guy Vigers, Ruth Aranda, Lars D. Engstrom, John P. Fischer, James G. Christensen, James F. Blake, Brian R. Baer, Josh Ballard, Vickie Bowcut
Publikováno v:
Molecular Cancer Therapeutics. 18:C069-C069
The ability to effectively target mutated KRAS has remained elusive despite decades of research. MRTX849 was identified via structure-based drug design as a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properti
Autor:
Ruth Aranda, Guy Vigers, James G. Christensen, John Fischer, Andrew Calinisan, Michael R. Burkhard, Lars D. Engstrom, Lauren Hargis, Fell Jay Bradford, David Briere, Matthew A. Marx, Peter D. Olson, Brian R. Baer, James F. Blake, Jill Hallin
Publikováno v:
Cancer Research. 79:LB-271
The ability to effectively target mutated KRAS has remained elusive despite decades of research. By solving a series of co-crystal structures coupled with iterative structure-based drug design, substituted tetrahydropyridopyrimidines were identified
Autor:
Vincent Leveque, Gloria Ao-Ieong, Sophie Le Pogam, Bamberg Joe Timothy, Javier de Vicente, Stengel Peter J, Stacey Renee Spencer, John P. Fischer, Todd R. Elworthy, Andrew J. Briggs, Jim Li, Peter Mohr, Michael Brandl, Sunil Sukhtankar, Ramona Hilgenkamp, Calvin Yee, Ludmila Alexandrova, Robinson John E, Fell Jay Bradford, Beihan Wang, April Wong, Robert Than Hendricks, Farrell Robert P, Isabel Najera, David Bernard Smith, Seth F. Harris, Sonal Rajyaguru, Susan Larrabee, James F. Blake, George Adjabeng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5652-5656
A series of benzo[d]isothiazole-1,1-dioxides were designed and evaluated as inhibitors of HCV polymerase NS5B. Structure-based design led to the incorporation of a high affinity methyl sulfonamide group. Structure-activity relationship (SAR) studies
Autor:
Elbert Chin, Manjiri Ghate, Vincent Leveque, Sonal Rajyaguru, Bill Fitch, Jahari Laurant Tracy, Michael Brandl, Steve A. de Keczer, Ramona Hilgenkamp, Fell Jay Bradford, Tatyana Voronin, Isabel Najera, Gloria Ao-Ieong, Javier de Vicente, Shao-Yong Wu, Beihan Wang, Stacey Renee Spencer, Stengel Peter J, Peter Mohr, Mohammad R. Masjedizadeh, James F. Blake, Robert Than Hendricks, Todd R. Elworthy, David Bernard Smith, Junping Zhao, Ludmila Alexandrova, Robinson John E, Al Lui, John P. Fischer, Seth F. Harris, Jim Li, Connie Oshiro, Calvin Yee, Sophie Le Pogam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5648-5651
Benzothiazine-substituted tetramic acids were discovered as highly potent non-nucleoside inhibitors of HCV NS5B polymerase. X-ray crystallography studies confirmed the binding mode of these inhibitors with HCV NS5B polymerase. Rational optimization o
Autor:
Stacey Renee Spencer, Vincent Leveque, Fell Jay Bradford, John A. Josey, Stengel Peter J, John P. Fischer, Robert Than Hendricks, April L. Bernacki, James F. Blake, Sophie Le Pogam, Sonal Rajyaguru, Steven Swallow, Robinson John E, Isabel Najera, Harris Jason R
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3637-3641
The importance of internal hydrogen bonding in a series of benzothiadiazine and 1,4-benzothiazine NS5b inhibitors has been explored. Computational analysis has been used to compare the protonated vs. anionic forms of each series and we demonstrate th
Autor:
Ludmila Alexandrova, Connie Oshiro, Ramona Hilgenkamp, Stengel Peter J, Isabel Najera, Peter Mohr, Jahari Laurant Tracy, Susan Larrabee, James F. Blake, David Bernard Smith, Bamberg Joe Timothy, George Adjabeng, Vincent Leveque, Andrew J. Briggs, Brian Xu, Seth F. Harris, Rebecca A. Stephenson, Sonal Rajyaguru, Manjiri Ghate, Beihan Wang, John P. Fischer, Stacey Renee Spencer, Calvin Yee, Sophie Le Pogam, Elbert Chin, Michael Brandl, Fell Jay Bradford, Gloria Ao-Ieong, Sunil Sukhtankar, Robert Than Hendricks, Jim Li, Robinson John E, Todd R. Elworthy, Farrell Robert P, Javier de Vicente
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3642-3646
A new series of benzothiazine-substituted quinolinediones were evaluated as inhibitors of HCV polymerase NS5B. SAR studies on this series revealed a methyl sulfonamide group as a high affinity feature. Analogues with this group showed submicromolar p
Autor:
Cheon Seung Hoon, Leonard J. Brand, Jeffrey Nadelson, Christina L. Leone, Rhonda O. Deems, Howard C. Smith, Douglas C. Knorr, Philip A. Bell, William S. Fillers, Thomas Daniel Aicher, Fell Jay Bradford, Ronald Simpson, Bork Balkan, Fraser James D, Gerald G. Kahle, Jiaping Gao
Publikováno v:
Journal of Medicinal Chemistry. 41:4556-4566
A series of substituted tetrahydropyrrolo[2,1-b]oxazol-5(6H)-ones and tetrahydropyrrolo[2,1-b]thiazol-5(6H)-ones was synthesized from amino alcohols or amino thiols and keto acids. A pharmacological model based on the results obtained with these comp