Publications by authors named "Guy Vigers"

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Conformation selection by ATP-competitive inhibitors and allosteric communication in ERK2.
Jake W Anderson, David Vaisar, David N Jones, Laurel M Pegram, Guy P Vigers

Elife· March 2024

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Conformation Selection by ATP-competitive Inhibitors and Allosteric Communication in ERK2.
Jake W Anderson, David Vaisar, David N Jones, Laurel M Pegram, Guy P Vigers

bioRxiv· November 2023

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Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS Inhibitor.
Xiaolun Wang, Shelley Allen, James F Blake, Vickie Bowcut, David M Briere, Guy P Vigers

J Med Chem· February 2022

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Identification of the Clinical Development Candidate , a Covalent KRAS Inhibitor for the Treatment of Cancer.
Jay B Fell, John P Fischer, Brian R Baer, James F Blake, Karyn Bouhana, Guy P Vigers

J Med Chem· July 2020

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The KRAS Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients.
Jill Hallin, Lars D Engstrom, Lauren Hargis, Andrew Calinisan, Ruth Aranda, Guy P Vigers

Cancer Discov· January 2020

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Activation loop dynamics are controlled by conformation-selective inhibitors of ERK2.
Laurel M Pegram, Jennifer C Liddle, Yao Xiao, Maria Hoh, Johannes Rudolph, Guy P Vigers

Proc Natl Acad Sci U S A· July 2019

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Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.
Jay B Fell, John P Fischer, Brian R Baer, Joshua Ballard, James F Blake, Guy P Vigers

ACS Med Chem Lett· December 2018

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8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.
Allen A Thomas, Kevin W Hunt, Brad Newhouse, Ryan J Watts, Xingrong Liu, Guy Vigers

J Med Chem· December 2014

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Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.
Matthew Volgraf, Lina Chan, Malcolm P Huestis, Hans E Purkey, Michael Burkard, Guy P A Vigers

Bioorg Med Chem Lett· June 2014

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Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.
Steve Wenglowsky, Li Ren, Jonas Grina, Joshua D Hansen, Ellen R Laird, Guy Vigers

Bioorg Med Chem Lett· April 2014

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Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease.
Yutong Jiang, Steven W Andrews, Kevin R Condroski, Brad Buckman, Vlad Serebryany, Guy Vigers

J Med Chem· March 2014

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Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.
Allen A Thomas, Kevin W Hunt, Matthew Volgraf, Ryan J Watts, Xingrong Liu, Guy Vigers

J Med Chem· February 2014

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Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.
Kevin W Hunt, Adam W Cook, Ryan J Watts, Christopher T Clark, Guy Vigers

J Med Chem· April 2013

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Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
James F Blake, Rui Xu, Josef R Bencsik, Dengming Xiao, Nicholas C Kallan, Guy P A Vigers

J Med Chem· September 2012

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An ATP-site on-off switch that restricts phosphatase accessibility of Akt.
Kui Lin, Jie Lin, Wen-I Wu, Joshua Ballard, Brian B Lee, Guy P A Vigers

Sci Signal· May 2012

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Non-oxime pyrazole based inhibitors of B-Raf kinase.
Bradley J Newhouse, Joshua D Hansen, Jonas Grina, Mike Welch, George Topalov, Guy Vigers

Bioorg Med Chem Lett· June 2011

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Discovery and SAR of spirochromane Akt inhibitors.
Nicholas C Kallan, Keith L Spencer, James F Blake, Rui Xu, Justin Heizer, Guy P A Vigers

Bioorg Med Chem Lett· April 2011

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Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.
Rui Xu, Anna Banka, James F Blake, Ian S Mitchell, Eli M Wallace, Guy P A Vigers

Bioorg Med Chem Lett· April 2011

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The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.
Alex J Buckmelter, Li Ren, Ellen R Laird, Bryson Rast, Greg Miknis, Guy Vigers

Bioorg Med Chem Lett· February 2011

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Non-oxime inhibitors of B-Raf(V600E) kinase.
Li Ren, Steve Wenglowsky, Greg Miknis, Bryson Rast, Alex J Buckmelter, Guy Vigers

Bioorg Med Chem Lett· February 2011

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Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.
Josef R Bencsik, Dengming Xiao, James F Blake, Nicholas C Kallan, Ian S Mitchell, Guy P A Vigers

Bioorg Med Chem Lett· December 2010

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Discovery of pyrrolopyrimidine inhibitors of Akt.
James F Blake, Nicholas C Kallan, Dengming Xiao, Rui Xu, Josef R Bencsik, Guy P A Vigers

Bioorg Med Chem Lett· October 2010

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Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition.
Wen-I Wu, Walter C Voegtli, Hillary L Sturgis, Faith P Dizon, Guy P A Vigers

PLoS One· September 2010

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RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.
Georgia Hatzivassiliou, Kyung Song, Ivana Yen, Barbara J Brandhuber, Daniel J Anderson, Guy Vigers

Nature· March 2010

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Potent and selective pyrazole-based inhibitors of B-Raf kinase.
Joshua D Hansen, Jonas Grina, Brad Newhouse, Mike Welch, George Topalov, Guy Vigers

Bioorg Med Chem Lett· August 2008

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