Zobrazeno 1 - 10
of 68
pro vyhledávání: '"John S. Tokarski"'
Autor:
Matthew D. Hill, Haiquan Fang, Derek Norris, George V. Delucca, Hong Huang, Mikkel DeBenedetto, Claude Quesnelle, William D. Schmitz, John S. Tokarski, Steven Sheriff, Chunhong Yan, Caroline Fanslau, Zuzana Haarhoff, Christine Huang, Melissa Kramer, Shilpa Madari, Krista Menard, Laura Monereau, John Morrison, Nirmala Raghavan, Eric E. Shields, Jean Simmermacher-Mayer, Michael Sinz, Ching Kim Tye, Richard Westhouse, Chunshan Xie, Haiying Zhang, Lisa Zhang, Tatyana Zvyaga, Francis Lee, Ashvinikumar V. Gavai, Andrew P. Degnan
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1165-1171
We describe the synthesis of triazole-containing carboline derivatives and their utility as bromodomain and extra-terminal (BET) inhibitors. A convergent synthetic route permitted the detailed investigation of deuteration and fluorination strategies
Autor:
Richard A. Hartz, Vijay T. Ahuja, Guanglin Luo, Ling Chen, Prasanna Sivaprakasam, Hong Xiao, Carol M. Krause, Wendy J. Clarke, Songmei Xu, John S. Tokarski, Kevin Kish, Hal Lewis, Nicolas Szapiel, Ramu Ravirala, Sayali Mutalik, Deepa Nakmode, Devang Shah, Catherine R. Burton, John E. Macor, Gene M. Dubowchik
Publikováno v:
Journal of Medicinal Chemistry.
Autor:
Ching Kim Tye, Chunhong Yan, Sarah C. Traeger, Wayne Vaccaro, Yingru Zhang, Gerry Everlof, Jianqing Li, Henry Yip, Peng Li, John T. Hunt, Michael A. Poss, Gregory D. Vite, Mussari Christopher P, Steven Sheriff, Asoka Ranasinghe, Haiying Zhang, Richard A. Westhouse, Dharmpal S. Dodd, Richard Rampulla, Zheng Yang, Frank Marsilio, Derek J. Norris, Wen-Ching Han, Tram N. Huynh, Yufen Zhao, Patrice Gill, Nirmala Raghavan, Lalgudi S. Harikrishnan, Ashvinikumar V. Gavai, Susan Wee, John S. Tokarski, Dauh-Rurng Wu, Arvind Mathur, Mei-Li Wen, Huiping Zhang, David R. Tortolani, George V. Delucca, Krista Menard, Francis Y. Lee, Claude A. Quesnelle, Dawn Sun, Vijay T. Ahuja, Daniel O'malley, Christine Huang, Muthoni G. Kamau
Publikováno v:
Journal of Medicinal Chemistry. 64:14247-14265
Inhibition of the bromodomain and extra-terminal (BET) family of adaptor proteins is an attractive strategy for targeting transcriptional regulation of key oncogenes, such as c-MYC. Starting with the screening hit 1, a combination of structure-activi
Autor:
Jonathan Lippy, Robert M. Borzilleri, Andrew J. Tebben, Litao Zhang, Charu Chaudhry, William J. Pitts, John S. Tokarski
Publikováno v:
Drug Discovery Today. 26:1115-1125
Kinases, accounting for 20% of the human genome, have been the focus of pharmaceutical drug discovery efforts for over three decades. Despite concerns surrounding the tractability of kinases as drug targets, it is evident that kinase drug discovery o
Autor:
Gregory A, Locke, Jodi, Muckelbauer, John S, Tokarski, Christopher M, Barbieri, Stefan, Belić, Bradley, Falk, Jeffrey, Tredup, Ying-Kai, Wang
Publikováno v:
Methods in enzymology. 667
Kinase inhibition continues to be a major focus of pharmaceutical research and discovery due to the central role of these proteins in the regulation of cellular processes. One family of kinases of pharmacological interest, due to its role in activati
Autor:
Jianqing Li, Daniel Smith, John S. Tokarski, Lihong Cheng, John E. Macor, Javed Khan, Adriana Zupa-Fernandez, Anil Thankappan, Chunjian Liu, Charu Chaudhry, David S. Weinstein, Percy H. Carter, Kathleen M. Gillooly, Kim W. McIntyre, Yifan Zhang, Anjaneya Chimalakonda, Joann Strnad, James Lin, James R. Burke, David J. Shuster, Manoj Chiney, Paul A. Elzinga, Max Ruzanov, Louis J. Lombardo, Charles M. Langevine
Publikováno v:
Journal of Medicinal Chemistry. 64:677-694
A search for structurally diversified Tyk2 JH2 ligands from 6 (BMS-986165), a pyridazine carboxamide-derived Tyk2 JH2 ligand as a clinical Tyk2 inhibitor currently in late development for the treatment of psoriasis, began with a survey of six-membere
Autor:
Gregory A. Locke, Jodi Muckelbauer, John S. Tokarski, Christopher M. Barbieri, Stefan Belić, Bradley Falk, Jeffrey Tredup, Ying-Kai Wang
Publikováno v:
Methods in Enzymology ISBN: 9780323915410
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0f1fcafaa9f16795bca7c80dddcc9f17
https://doi.org/10.1016/bs.mie.2022.03.051
https://doi.org/10.1016/bs.mie.2022.03.051
Autor:
Andrew P. Degnan, Haiquan Fang, Tatyana Zvyaga, Zuzana Haarhoff, Claude A. Quesnelle, Melissa Kramer, Frank Marsilio, Richard A. Westhouse, John S. Tokarski, Shilpa Madari, Jiuqiao Zhao, Amy Wiebesiek, Chunhong Yan, Francis Y. Lee, Michael Sinz, John Morrison, Jean Simmermacher-Mayer, Carolynn Fanslau, Steven Sheriff, Lisa Huang, Ashvinikumar V. Gavai, Chunshan Xie, Matthew D. Hill, Gerry Everlof
Publikováno v:
Bioorganicmedicinal chemistry letters. 51
We describe our efforts to introduce structural diversity to a previously described triazole-containing N1-carboline series of bromodomain and extra-terminal (BET) inhibitors. N9 carbolines were designed to retain favorable binding interactions that
Autor:
Ashvinikumar V. Gavai, Brian E. Fink, Dianlin Xie, Susan Wee, David A Critton, Jesse Swanson, Carolyn Cao, John S. Tokarski, Vijay T. Ahuja, Daniel O'malley, Nicolas Szapiel, Benjamin M. Johnson, Cindy Wang, Anthony A. Paiva
Publikováno v:
ACS Medicinal Chemistry Letters. 10:1486-1491
C-terminal Src kinase (CSK) functions as a negative regulator of T cell activation through inhibitory phosphorylation of LCK, so inhibitors of CSK are of interest as potential immuno-oncology agent...
Autor:
Charu Chaudhry, Percy H. Carter, Moslin Ryan M, Celia D’Arienzo, James Lin, Jodi K. Muckelbauer, Luisa Salter-Cid, Tracy L. Taylor, Kim W. McIntyre, Chunjian Liu, James R. Burke, Paul A. Elzinga, Hyunsoo Park, Kathleen M. Gillooly, Chiehying Chang, Dianlin Xie, Jing Chen, Lihong Cheng, David S. Weinstein, Cliff Chen, Jeffrey Tredup, Huadong Sun, Peng Li, Louis J. Lombardo, Adriana Zupa-Fernandez, Joann Strnad, John S. Tokarski, Dauh-Rurng Wu, Nelly Aranibar
Publikováno v:
ACS Medicinal Chemistry Letters. 10:383-388
In sharp contrast to a previously reported series of 6-anilino imidazopyridazine based Tyk2 JH2 ligands, 6-((2-oxo-N1-substituted-1,2-dihydropyridin-3-yl)amino)imidazo[1,2-b]pyridazine analogs were found to display dramatically improved metabolic sta