Zobrazeno 1 - 10
of 41
pro vyhledávání: '"Guy Vigers"'
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:
Natalie G. Ahn, Weiru Wang, Yao Xiao, Dylan B. Iverson, Jennifer C Liddle, Darin Smith, Laurel M. Pegram, John Moffat, Johannes Rudolph, Hailong Zhang, Guy Vigers, Maria Hoh
Modulating the dynamics of protein kinases expands the inhibitory mechanisms for small molecules. NMR measurements of the MAP kinase, ERK2, have shown that activation by dual-phosphorylation induces global motions involving exchange between two state
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2909655df3e646e80c162cc60476973e
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:
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:
Victoria Dinkel, Jonas Grina, David A. Moreno, Simon Mathieu, Joshua D. Hansen, Kevin Rasor, Gregg Hastings, Walter C. Voegtli, Guy Vigers, Sumeet Rana, Joachim Rudolph, Susan L. Gloor, Ellen R. Laird, Li Ren, Steve Wenglowsky, Brandon S. Willis, Hillary L. Sturgis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1923-1927
Herein we describe the design of a novel series of ATP competitive B-Raf inhibitors via structure-based methods. These 3-N-methylquinazoline-4(3H)-one based inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimizati
Autor:
Darin Smith, Guy Vigers, Sumeet Rana, Michael Burkard, April Cox, Robert D. Groneberg, Ryan J. Watts, Robert Kirk Delisle, Tony Pisal Tang, Andrew T. Metcalf, Kelly Regal, Susan P. Rhodes, Mary K. Geck Do, Karin D. Brown, Joseph P. Lyssikatos, Douglas Mccord Sammond, Matthew Volgraf, Albion D. Wright, Gunawardana Indrani W, Kimberly Scearce-Levie, Jennifer N. Otten, Allen A. Thomas, Michael Siu, Hans E. Purkey, Kevin W. Hunt, Xingrong Liu, Darrin Dutcher
Publikováno v:
Journal of Medicinal Chemistry. 57:878-902
In an attempt to increase selectivity vs Cathepsin D (CatD) in our BACE1 program, a series of 1,3,4,4a,10,10a-hexahydropyrano[4,3-b]chromene analogues was developed. Three different Asp-binding moieties were examined: spirocyclic acyl guanidines, ami
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:
Kevin W. Hunt, Darin Smith, Weiru Wang, Matthew Volgraf, Guy Vigers, Michael Siu, Darrin Dutcher, Hans E. Purkey, Christine Yu, Liu Wendy, Malcolm P. Huestis
Publikováno v:
Tetrahedron Letters. 54:5802-5807
A series of unique bicyclic aminooxazolines were synthesized and found to exhibit micromolar inhibition of β-secretase-1 (BACE-1). The aminooxazolines were procured by an intramolecular diethylaminosulfur trifluoride (DAST)-mediated ring closure of
Autor:
Leonid Beigelman, Hailong Zhang, Benjamin T. Woodard, Christine Lemieux, Guy Vigers, Vlad Serebryany, Brad O. Buckman, Bin Wang, Scott D. Seiwert, Barbra J. Brandhuber, Steve Wenglowsky, Stengel Peter J, Andrews Steven W, Lawrence M. Blatt, Kennedy April L, Doherty George Andrew, John A. Josey, Joshua Ballard, Mary Geck Do, Madduru Machender R, Jiang Yutong, Kevin Ronald Condroski, Michael Lyon
Publikováno v:
Journal of Medicinal Chemistry. 57:1753-1769
HCV serine protease NS3 represents an attractive drug target because it is not only essential for viral replication but also implicated in the viral evasion of the host immune response pathway through direct cleavage of key proteins in the human inna
Autor:
Josef R. Bencsik, Barbara J. Brandhuber, Banka Anna L, Guy Vigers, Nicholas J. Skelton, Stefan D. Gross, Wen-I Wu, Matthew Martinson, Ian S. Mitchell, Susan L. Gloor, Rui Xu, Keith Lee Spencer, Tyler Risom, James F. Blake, Nicholas C. Kallan, Eli M. Wallace, Tony Morales
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2335-2340
We describe the design and synthesis of novel bicyclic spiro sulfonamides as potent Akt inhibitors. Through structure-based rational design, we have successfully improved PKA selectivity of previously disclosed spirochromanes. Representative compound