Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Mary-Ellen Banker"'
Autor:
Martin E. Dowty, James F. Smith, Tsung H. Lin, Brian S. Gerstenberger, Matthew C. Griffor, Brett D. Hollingshead, Roger S. Gifford, Martin Hegen, Felix Vajdos, John D. Knafels, Andrew Fensome, Mary Ellen Banker, James D. Clark
Publikováno v:
Scientific Reports, Vol 10, Iss 1, Pp 1-9 (2020)
Scientific Reports
Scientific Reports
Translation of modulation of drug target activity to therapeutic effect is a critical aspect for all drug discovery programs. In this work we describe the profiling of a non-receptor tyrosine-protein kinase (TYK2) inhibitor which shows a functionally
Autor:
Dafydd R. Owen, James D. Clark, Xiaojing Yang, Eddine Saiah, Martin Hegen, Brian S. Gerstenberger, Felix Vajdos, Catherine M. Ambler, Li Xing, Alpay Dermenci, Tsung H. Lin, Matthew Merrill Hayward, Raman Sharma, Xin Yang, David W. Lin, John D. Knafels, Eric P. Arnold, Mary-Ellen Banker, Stephen W. Wright, Martin E. Dowty, Brett D. Hollingshead, Andrew Fensome, Susan Fish, Matthew Frank Brown
Publikováno v:
Journal of medicinal chemistry. 63(22)
Tyrosine kinase 2 (TYK2) is a member of the JAK kinase family that regulates signal transduction downstream of receptors for the IL-23/IL-12 pathways and type I interferon family, where it pairs with JAK2 or JAK1, respectively. On the basis of human
Autor:
Brett D. Hollingshead, Fabien Vincent, Tsung H. Lin, John I. Trujillo, Betsy Pierce, Andrew Fensome, Brian S. Gerstenberger, Martin E. Dowty, Matthew Frank Brown, Xin Yang, David C. Limburg, Martin Hegen, John D. Knafels, Felix Vajdos, Andrew C. Flick, Mary Ellen Banker, Raman Sharma, Li Xing, Jason Jussif, Catherine M. Ambler, Ivan Viktorovich Efremov, James D. Clark, Liying Zhang, Peter T. Symanowicz, Eddine Saiah, Jill Chrencik, Jean-Baptiste Telliez, Xiaojing Yang, Eric P. Arnold, Ariamala Gopalsamy, Zhao-Kui Wan, Matthew Merrill Hayward, David W. Lin
Publikováno v:
Journal of Medicinal Chemistry. 61:8597-8612
Cytokine signaling is an important characteristic of autoimmune diseases. Many pro-inflammatory cytokines signal through the Janus kinase (JAK)/Signal transducer and activator of transcription (STAT) pathway. JAK1 is important for the γ-common chain
Autor:
Seungil Han, Martin E. Dowty, Ralph P. Robinson, Steven E. Heasley, Peter T. Symanowicz, Jason Jussif, Thomas M. Harris, Neelu Kaila, Lu Wang, Matthew Frank Brown, Jeffrey M. Casavant, Nicole Caspers, Sarah H. Griffin, Mark J. Mitton-Fry, Martin Hegen, Johnson Timothy Allan, Tenbrink Ruth E, Mary Ellen Banker, Jonathan Langille, Mihir D. Parikh, Tsung H. Lin, Arindrajit Basak, Jean-Baptiste Telliez, James D. Clark, Strohbach Joseph Walter, Eric P. Arnold, Ray Unwalla, Li Li, Brian A. Duclos, Xin Yang, Mark Edward Flanagan, John David Trzupek, Michael L. Vazquez, Soojin Kwon, Ashley Edward Fenwick
Publikováno v:
Journal of Medicinal Chemistry. 61:1130-1152
Janus kinases (JAKs) are intracellular tyrosine kinases that mediate the signaling of numerous cytokines and growth factors involved in the regulation of immunity, inflammation, and hematopoiesis. As JAK1 pairs with JAK2, JAK3, and TYK2, a JAK1-selec
Autor:
Kentaro Futatsugi, Mary Ellen Banker, David W. Piotrowski, Kun Song, Michael Herr, Jonathan N. Bauman, Steven B Co, Sophie Y. Lavergne, Stephen W. Wright, Paula M. Loria, Liuqing Wei, Agustin Casimiro-Garcia, Wenhua Jiao, Matthew F. Sammons, Donna N. Petersen
Publikováno v:
Journal of Medicinal Chemistry. 61:1086-1097
A novel series of morpholine-based nonsteroidal mineralocorticoid receptor antagonists is reported. Starting from a pyrrolidine HTS hit 9 that possessed modest potency but excellect selectivity versus related nuclear hormone receptors, a series of li
Autor:
Robert M. Czerwinski, Mary Ellen Banker, Paul Balbo, Atli Thorarensen, Jean-Baptiste Telliez, Max Kuhn, Arthur J. Wittwer, Tristan S. Maurer, Fabien Vincent
Publikováno v:
Bioorganic & Medicinal Chemistry. 29:115865
Recent years have seen a resurgence in drug discovery efforts aimed at the identification of covalent inhibitors which has led to an explosion of literature reports in this area and most importantly new approved therapies. These reports and breakthro
Autor:
David C. Limburg, Andrew Fensome, Fabien Vincent, Betsy Pierce, Martin E. Dowty, Mary Ellen Banker, Raman Sharma, Xin Yang, Ariamala Gopalsamy, Roger S. Gifford, Brian S. Gerstenberger, Andrew C. Flick, Eric P. Arnold, Jason Jussif, Ivan Viktorovich Efremov, Xiaojing Yang, Martin Hegen, Zhao-Kui Wan, Felix Vajdos, Catherine M. Ambler, James D. Clark, Tsung H. Lin, John I. Trujillo, Li Xing
Publikováno v:
Bioorganic & Medicinal Chemistry. 28:115481
Herein, we disclose a new series of TYK2/ JAK1 inhibitors based upon a 3.1.0 azabicyclic substituted pyrimidine scaffold. We illustrate the use of structure-based drug design for the initial design and subsequent optimization of this series of compou
Autor:
Andrew, Fensome, Catherine M, Ambler, Eric, Arnold, Mary Ellen, Banker, Matthew F, Brown, Jill, Chrencik, James D, Clark, Martin E, Dowty, Ivan V, Efremov, Andrew, Flick, Brian S, Gerstenberger, Ariamala, Gopalsamy, Matthew M, Hayward, Martin, Hegen, Brett D, Hollingshead, Jason, Jussif, John D, Knafels, David C, Limburg, David, Lin, Tsung H, Lin, Betsy S, Pierce, Eddine, Saiah, Raman, Sharma, Peter T, Symanowicz, Jean-Baptiste, Telliez, John I, Trujillo, Felix F, Vajdos, Fabien, Vincent, Zhao-Kui, Wan, Li, Xing, Xiaojing, Yang, Xin, Yang, Liying, Zhang
Publikováno v:
Journal of medicinal chemistry. 61(19)
Cytokine signaling is an important characteristic of autoimmune diseases. Many pro-inflammatory cytokines signal through the Janus kinase (JAK)/Signal transducer and activator of transcription (STAT) pathway. JAK1 is important for the γ-common chain
Autor:
Louis Leung, Jonathan Langille, John I. Trujillo, Paul B. Balbo, Jason Jussif, Jill Chrencik, Martin Hegen, Felix Vajdos, Atli Thorarensen, Sarah Soucy, Adam M. Gilbert, Jean-Baptiste Telliez, Tsung Lin, Ray Unwalla, Matthew Merrill Hayward, Justin I. Montgomery, Sidney Liang, Fabien Vincent, Robert M. Czerwinski, Ye Che, Martin E. Dowty, Mary Ellen Banker, Xin Yang, Matthew Frank Brown, Agustin Casimiro-Garcia, Jotham Wadsworth Coe, Brian Juba
Publikováno v:
Journal of medicinal chemistry. 60(5)
Significant work has been dedicated to the discovery of JAK kinase inhibitors resulting in several compounds entering clinical development and two FDA approved NMEs. However, despite significant effort during the past 2 decades, identification of hig
Autor:
Li Xing, Jane M. Withka, Guoyun Bai, Mark E. Bunnage, Bruce Allen Lefker, Leslie Anthony Dakin, Sheng Tan, Shenping Liu, Mary Ellen Banker, Parag Sahasrabudhe, Ariamala Gopalsamy, Atli Thorarensen, Hua Xu, Jennifer A. Young, Joerg Bussenius, Boris A. Chrunyk, Jinshan M. Chen, Kieran F. Geoghegan, Stephen W. Wright, Suman Shanker, Jeremy T. Starr, Paul Balbo, Xiayang Qiu, Zuojun Guo, Wei Li, Lyn H. Jones, Fabien Vincent, Lise R. Hoth
Publikováno v:
Scientific Reports
Interleukin-17A (IL-17A) is a principal driver of multiple inflammatory and immune disorders. Antibodies that neutralize IL-17A or its receptor (IL-17RA) deliver efficacy in autoimmune diseases, but no small-molecule IL-17A antagonists have yet progr