Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Matthew Martinson"'
Autor:
Jill Hallin, Vickie Bowcut, Andrew Calinisan, David M. Briere, Lauren Hargis, Lars D. Engstrom, Jade Laguer, James Medwid, Darin Vanderpool, Ella Lifset, David Trinh, Natalie Hoffman, Xiaolun Wang, J. David Lawson, Robin J. Gunn, Christopher R. Smith, Nicole C. Thomas, Matthew Martinson, Alex Bergstrom, Francis Sullivan, Karyn Bouhana, Shannon Winski, Leo He, Julio Fernandez-Banet, Adam Pavlicek, Jacob R. Haling, Lisa Rahbaek, Matthew A. Marx, Peter Olson, James G. Christensen
Publikováno v:
Nature Medicine. 28:2171-2182
Autor:
James Christensen, Jill Hallin, Vickie Bowcut, Andrew Calinisan, David Briere, Lauren Hargis, Lars Engstrom, Jade Laguer, James Medwid, Darin Vanderpool, Ella Lifset, David Trinh, Natalie Hoffman, Xiaolun Wang, J. Lawson, Robin Gunn, Christopher Smith, Nicole Thomas, Matthew Martinson, Alex Bergstrom, Francis Sullivan, Karyn Bouhana, Shannon Winski, Leo He, Fernandez-Banet Julio, Adam Pavlicek, Jacob Haling, Lisa Rahbaek, Matthew Marx, Peter Olson
The ability to effectively target mutated KRAS has remained elusive despite decades of research. The recent identification of KRASG12C inhibitors has provided an effective treatment option for patients harboring this particular mutation and has also
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::10fbcfa8cb41321f46bb73555a3d1e2c
https://doi.org/10.21203/rs.3.rs-1261963/v1
https://doi.org/10.21203/rs.3.rs-1261963/v1
Autor:
Jill, Hallin, Vickie, Bowcut, Andrew, Calinisan, David M, Briere, Lauren, Hargis, Lars D, Engstrom, Jade, Laguer, James, Medwid, Darin, Vanderpool, Ella, Lifset, David, Trinh, Natalie, Hoffman, Xiaolun, Wang, J, David Lawson, Robin J, Gunn, Christopher R, Smith, Nicole C, Thomas, Matthew, Martinson, Alex, Bergstrom, Francis, Sullivan, Karyn, Bouhana, Shannon, Winski, Leo, He, Julio, Fernandez-Banet, Adam, Pavlicek, Jacob R, Haling, Lisa, Rahbaek, Matthew A, Marx, Peter, Olson, James G, Christensen
Publikováno v:
Nature medicine. 28(10)
Recent progress in targeting KRAS
Autor:
Michael Burkard, Andrew T. Metcalf, Kristina West, Stephen E. Gould, Matthew Martinson, John Moffat, Kevin Rasor, Weiru Wang, Li Ren, Jacob Schwarz, Sheerin K. Shahidi-Latham, Patricia Pacheco, Huifen Chen, Jianping Yin, Jonas Grina, David A. Moreno, Rustam Ferdinand Garrey, James F. Blake, John Gaudino, Brian Dean
Publikováno v:
Journal of Medicinal Chemistry. 58:1976-1991
Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was developed. Optimization led to the identification of (S)-14k, a potent, selective, and orally bioavailable agent that inhibited tumor growth in mouse xenograft models. On
Autor:
John Moffat, Marcia Belvin, Lichuan Liu, Jocelyn Chan, Li Ren, Kirk Robarge, Francis J. Sullivan, Jeffrey Stults, Jonas Grina, David A. Moreno, Ann Qin, Matthew Martinson, Stephen E. Gould, Jacob Schwarz, Kang-Jye Chou, Sheerin K. Shahidi-Latham, Lars Mueller, John Gaudino, Aihe Zhou, James F. Blake, Weiru Wang, Danette Dudley, Christine Orr, Michael Burkard, Thomas Hunsaker, Dolores Diaz, Mark Merchant, Huifen Chen, Jianping Yin, Patricia Pacheco, Kevin Rasor
Publikováno v:
Journal of medicinal chemistry. 59(12)
The extracellular signal-regulated kinases ERK1/2 represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that is commonly activated by oncogenic mutations in BRAF or RAS or by upstream oncogenic signaling. While targeting upstream n
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
Autor:
Nicholas J. Skelton, Matthew Martinson, Ian S. Mitchell, Josef R. Bencsik, Susan L. Gloor, Tony Morales, Rui Xu, Keith Lee Spencer, Tyler Risom, Barbara J. Brandhuber, Guy Vigers, Nicholas C. Kallan, Justin W. Heizer, James F. Blake, Wen-I Wu, Stefan D. Gross
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2410-2414
A novel series of spirochromane pan-Akt inhibitors is reported. SAR optimization furnished compounds with improved enzyme potencies and excellent selectivity over the related AGC kinase PKA. Attempted replacement of the phenol hinge binder provided c
Autor:
Bryson Rast, Alexandre J. Buckmelter, Li Ren, Walter C. Voegtli, Greg Miknis, Robert J. Ely, Tony Morales, Guy Vigers, Nikole Randolph, Ellen R. Laird, Michele Callejo, Joseph P. Lyssikatos, Sarah Galbraith, Matthew Martinson, Stephen T. Schlachter, Barbara J. Brandhuber, Steve Wenglowsky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1243-1247
The development of inhibitors of B-Raf(V600E) serine-threonine kinase is described. Various head-groups were examined to optimize inhibitor activity and ADME properties. Several of the head-groups explored, including naphthol, phenol and hydroxyamidi
Autor:
Keith Lee Spencer, Tyler Risom, Guy Vigers, Nicholas J. Skelton, Stefan D. Gross, Nicholas C. Kallan, Josef R. Bencsik, James F. Blake, Matthew Martinson, Ian S. Mitchell, Rui Xu, Richard Woessner, Tony Morales, Susan L. Gloor, Dengming Xiao, Barbara J. Brandhuber
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5607-5612
The discovery and optimization of a series of pyrrolopyrimidine based protein kinase B (Pkb/Akt) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent inhibition of all three Akt isoforms and knoc
Autor:
Barbara J. Brandhuber, George T. Topalov, Michele Callejo, Matthew Martinson, Nikole Randolph, Susan L. Gloor, Ellen R. Laird, Brad Newhouse, Mike Welch, Joseph P. Lyssikatos, Joshua D. Hansen, Jonas Grina, Rich Woessner, Alan G. Olivero, Guy Vigers, Nicole M Littman, Tony Morales
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4692-4695
Herein we describe a novel pyrazole-based class of ATP competitive B-Raf inhibitors. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. A subset of these inhibitors has demonstrated the ability to inhibit downstr