Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Scott Jakes"'
Autor:
Steven Kerr, Charles L. Cywin, Frank H. Büttner, Frank Wu, Mohammed A. Kashem, Scott Jakes, Zofia Paw, Roger J. Snow, Erick R. R. Young, Eugene R. Hickey, Stanley Kugler, Paul Kaplita, Cheng-Kon Shih, Rhonda Chen, Anthony S. Prokopowicz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3235-3239
Two closely related scaffolds were identified through an uHTS campaign as desirable starting points for the development of Rho-Kinase (ROCK) inhibitors. Here, we describe our hit-to-lead evaluation process which culminated in the rapid discovery of p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c2d691a0169d6458e981f329be40c8b
https://doi.org/10.1016/j.bmcl.2010.04.070
https://doi.org/10.1016/j.bmcl.2010.04.070
Autor:
Eugene R. Hickey, Anthony S. Prokopowicz, George E. Lee, Carol Ann Homon, Scott Jakes, Wang Mao, Jun Li, Charlene Peng, Bennett T. Farmer, Scott F. Leonard, Mohammed A. Kashem, Kevin Chungeng Qian, Charles L. Cywin, Lian Wang, Ronald Magboo, Morgan Welzel, John P. Wolak, Edward Pack, Tina Morwick
Publikováno v:
Journal of Medicinal Chemistry. 52:1814-1827
A series of inhibitors of Pim-2 kinase identified by high-throughput screening is described. Details of the hit validation and lead generation process and structure-activity relationship (SAR) studies are presented. Disclosure of an unconventional bi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40bdff6788836da6a99ef9f5bd96cab0
https://doi.org/10.1021/jm801242y
https://doi.org/10.1021/jm801242y
Autor:
Axel Knebel, Charline Peng, Brian Werneburg, Xiang Li, Scott Jakes, Kevin Barringer, Jun Li, Lian Wang, Nick A. Morrice
Publikováno v:
Journal of Biochemistry. 141:353-362
The Pim family of Ser/Thr kinases has been implicated in the process of lymphomagenesis and cell survival. Known substrates of Pim kinases are few and poorly characterized. In this study we set out to identify novel Pim-2 substrates using the Kinase
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::97157313f740542d3bb6e3e2b03b7699
https://doi.org/10.1093/jb/mvm040
https://doi.org/10.1093/jb/mvm040
Autor:
Walter Davidson, Scott Jakes, Susan Lukas, Gregory W. Peet, Christopher Pargellis, Roger J. Snow, Rachel R. Kroe, Lee Frego, Mark E. Labadia, Brian Werneburg, Christine A. Grygon
Publikováno v:
Biochemistry. 43:11658-11671
A novel inhibitor of p38 mitogen-activated protein kinase (p38), CMPD1, identified by high-throughput screening, is characterized herein. Unlike the p38 inhibitors described previously, this inhibitor is substrate selective and noncompetitive with AT
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d621e78115b26c6a3eff01628a61a09
https://doi.org/10.1021/bi0495073
https://doi.org/10.1021/bi0495073
Publikováno v:
Molecular Immunology. 40:681-694
Signaling through the CD40 receptor activates diverse molecular pathways in a variety of immune cell types. To study CD40 signaling complexes in B cells, we produced soluble CD40 cytoplasmic domain multimers that translocate across cell membranes and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6cb1a13227b988f233d86a0662b4a80d
https://doi.org/10.1016/j.molimm.2003.09.003
https://doi.org/10.1016/j.molimm.2003.09.003
Autor:
Daniel R. Goldberg, Mark A. Bobko, Bao-Ping Zhao, Charles L. Cywin, Mohammed A. Kashem, Richard Soll, Amy Gao, Anthony S. Prokopowicz, Mcneil Daniel W, Mark R. Player, Rinker James M, Ronald L. Magolda, Matt Hrapchak, Renee L. DesJarlais, Michael P. Winters, Scott Jakes, Tina Morwick
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1415-1418
The discovery of novel 5,7-disubstituted[1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK) is discussed. The SAR reveals the necessity for a 7-aryl group with preference towards para substitution and that this in combination wit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6435bde3139c578deebc55c9fcdb0c6a
https://doi.org/10.1016/s0960-894x(03)00163-x
https://doi.org/10.1016/s0960-894x(03)00163-x
Discovery of 2-Phenylamino-imidazo[4,5-h]isoquinolin-9-ones: A New Class of Inhibitors of Lck Kinase
Autor:
Maret Panzenbeck, Mario G. Cardozo, Robert M. Tolbert, Jeffrey D. Peterson, Susan Lukas, Stephen Jacober, Robert J. Eckner, Gregory W. Peet, Anthony S. Prokopowicz, Carl A. Busacca, Suresh R. Kapadia, Scott Jakes, Tina Morwick, Roger J. Snow, Rosemarie Sellati, Yong Dong, Matt Aaron Tschantz, Neil Moss
Publikováno v:
Journal of Medicinal Chemistry. 45:3394-3405
An imidazo[4,5-h]isoquinolin-7,9-dione (1) was identified as an adenosine 5'-triphosphate competitive inhibitor of lck by high throughput screening. Initial structure-activity relationship studies identified the dichlorophenyl ring and the imide NH a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcb66ed0ff6ce36eb079aaec851fb78a
https://doi.org/10.1021/jm020113o
https://doi.org/10.1021/jm020113o
Publikováno v:
The Journal of Immunology. 164:5199-5206
Lnk was originally cloned from a rat lymph node cDNA library and shown to participate in T cell signaling. Human Lnk (hLnk) was cloned by screening a Jurkat cell cDNA library. hLnk has a calculated molecular mass of 63 kDa, and its deduced amino acid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a5682917d4c9f122245a9474a286150
https://doi.org/10.4049/jimmunol.164.10.5199
https://doi.org/10.4049/jimmunol.164.10.5199
Autor:
Jean Rancourt, Kirrane Thomas M, Rajiv Sharma, Martin Poirier, John R. Proudfoot, Susan Lukas, Montse Llinas-Brunet, Usha R. Patel, Dominik Wernic, Alisa K. Kabcenell, Pierre L. Beaulieu, Neil Moss, Scott Jakes, Vida Gorys, Jean Gauthier, Mario G. Cardozo, Liang Tong, Eugene R. Hickey, Dale R. Cameron, Jean-Marie Ferland, Raj Betageri, Richard H. Ingraham, James Gillard, Ghiro Elise
Publikováno v:
Journal of Medicinal Chemistry. 42:1757-1766
p56lck is a member of the src family of tyrosine kinases. Through modular binding units called SH2 domains, p56lck promotes phosphotyrosine-dependent protein-protein interactions and plays a critical role in signal transduction events that lead to T-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7ffbdfc7ecc758ac0b4b9d5f4856b0c
https://doi.org/10.1021/jm980676t
https://doi.org/10.1021/jm980676t
Autor:
Randall W. Barton, Josephine Schembri-King, Thomas C. Warren, Gregory W. Peet, Marilyn Kehry, Jun Li, Steven S. Pullen, Kenneth B. Marcu, Scott Jakes
Publikováno v:
Journal of Biological Chemistry. 273:30736-30741
Activation of the transcription factor NF-κB is regulated by the phosphorylation and subsequent degradation of its inhibitory subunit, IκB. A large multiprotein complex, the IκB kinase (IKK), catalyzes the phosphorylation of IκB. The two kinase c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bbabc14b5ccad59ee6794915af347b99
https://doi.org/10.1074/jbc.273.46.30736
https://doi.org/10.1074/jbc.273.46.30736