Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Tsung H, Lin"'
Autor:
Martin E. Dowty, Tsung H. Lin, Michael I. Jesson, Martin Hegen, David A. Martin, Vaibhav Katkade, Sujatha Menon, Jean‐Baptiste Telliez
Publikováno v:
Pharmacology Research & Perspectives, Vol 7, Iss 6, Pp n/a-n/a (2019)
Abstract Janus kinase (JAK) inhibitors have emerged as an effective class of therapies for various inflammatory diseases such as rheumatoid arthritis (RA). JAK inhibitors function intracellularly by modulating the catalytic activity of JAKs and disru
Externí odkaz:
https://doaj.org/article/f3050391c79d4c7b80c8e2996dc077c2
Autor:
Jonathan N. Bauman, Angela C. Doran, Amanda King-Ahmad, Raman Sharma, Gregory S. Walker, Jian Lin, Tsung H. Lin, Jean-Baptiste Telliez, Sakambari Tripathy, Theunis C. Goosen, Christopher Banfield, Bimal K. Malhotra, Martin E. Dowty
Publikováno v:
Drug Metabolism and Disposition. 50:1106-1118
Abrocitinib is an oral once-daily Janus kinase 1 selective inhibitor being developed for the treatment of moderate-to-severe atopic dermatitis. This study examined the disposition of abrocitinib in male participants following oral and intravenous adm
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::926208d526384181f37cc80f92c02aa6
https://doi.org/10.1124/dmd.122.000829
https://doi.org/10.1124/dmd.122.000829
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2666dee375aa129903ab5f908c84a04a
http://link.springer.com/article/10.1038/s41598-020-65762-y
http://link.springer.com/article/10.1038/s41598-020-65762-y
Autor:
Iain Kilty, Uthpala Seneviratne, M Nusrat Sharif, Gary R. Point, Jean-Baptiste Telliez, Tsung H. Lin, Douglas S. Johnson, Michael I. Jesson, John I. Trujillo, Chuong Nguyen, Hua Xu, Liang Xue, Robert A. Everley, Atli Thorarensen
Publikováno v:
ACS Chemical Biology. 14:1235-1242
PF-06651600 was developed as an irreversible inhibitor of JAK3 with selectivity over the other three JAK isoforms. A high level of selectivity toward JAK3 is achieved by the covalent interaction of PF-06651600 with a unique cysteine residue (Cys-909)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32ed51fa955664495a184af61925bde2
https://doi.org/10.1021/acschembio.9b00188
https://doi.org/10.1021/acschembio.9b00188
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62513b08e1117b54db6ce345e9512f36
https://pubmed.ncbi.nlm.nih.gov/32787094
https://pubmed.ncbi.nlm.nih.gov/32787094
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4d4f153dbb8b5bb68fb24a9742305143
https://doi.org/10.1021/acs.jmedchem.8b00917
https://doi.org/10.1021/acs.jmedchem.8b00917
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73b9d013c1aa57b2199cce24ad33fac0
https://doi.org/10.1021/acs.jmedchem.7b01598
https://doi.org/10.1021/acs.jmedchem.7b01598
Publikováno v:
Signaling through Cell Abhesion Molecules
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::db7fb3d70bcab5f48a00c21116e4e966
https://doi.org/10.1201/9780429129384-8
https://doi.org/10.1201/9780429129384-8
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc4d8bef6390fa6ece1b44635a741fad
https://doi.org/10.1016/j.bmc.2020.115481
https://doi.org/10.1016/j.bmc.2020.115481
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::ad2ad9462488003d246ff771f1250154
https://pubmed.ncbi.nlm.nih.gov/30113844
https://pubmed.ncbi.nlm.nih.gov/30113844