Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Strohbach Joseph Walter"'
Autor:
Jeanne Chang, Ravi G. Kurumbail, Margaret Fleming, Joanne Brodfuehrer, Katherine L. Lee, Frank Lovering, Shashi Mohan, Heather V. Dowty, Fabien Vincent, Jayasankar Jasti, Steve Kortum, Christoph W. Zapf, Jotham Wadsworth Coe, Christophe Allais, Strohbach Joseph Walter, Nikolaos Papaioannou, Ann Aulabaugh, Julia A. Guzova, Paul Morgan, Richard K. Frisbie, WeiDong Ding, David Hepworth
Publikováno v:
European Journal of Medicinal Chemistry. 145:606-621
Many diseases are believed to be driven by pathological levels of reactive oxygen species (ROS) and oxidative stress has long been recognized as a driver for inflammatory disorders. Apoptosis signal-regulating kinase 1 (ASK1) has been reported to be
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:
Brian Juba, Betsy Pierce, Steve Kortum, Armon Sharei, Jing Li, Erik C. Hett, Jean-Baptiste Telliez, Bu Wang, Mark E. Bunnage, Lee R. Roberts, Strohbach Joseph Walter, Michael Pacheco, Atli Thorarensen, Lyn H. Jones, Michael L. Vazquez, Jonathan B. Gilbert
Publikováno v:
ACS Chemical Biology. 12:2970-2974
Biochemical screening is a major source of lead generation for novel targets. However, during the process of small molecule lead optimization, compounds with excellent biochemical activity may show poor cellular potency, making structure-activity rel
Autor:
Lori Krim Gavrin, David Hepworth, Jennifer R. Thomason, Iain Kilty, Joel Adam Goldberg, Christoph W. Zapf, Vikram R. Rao, Brian P. Boscoe, Akshay Patny, Peter T. Symanowicz, Marina W.H. Shen, Kevin J. Curran, Elizabeth Murphy, Martin Hegen, Fabien Vincent, Richard Vargas, Satwik Kamtekar, Heidi M. Morgan, Heidi R. Hope, Richard K. Frisbie, Jeanne S. Chang, Ken Dower, Susan E. Drozda, Strohbach Joseph Walter, Mathias John Paul, David R. Anderson, Jacqueline E. Day, Stephen W. Wright, Ivan J. Samardjiev, Seungil Han, Julia H Shin, Frank Lovering, Andrea G Bree, Arthur Lee, Holly H. Soutter, Joanne Brodfuehrer, John David Trzupek, Brian Samas, Christoph Martin Dehnhardt, Michael Dennis Lowe, Catherine M. Ambler, Seung Won Chung, Eddine Saiah, Nikolaos Papaioannou, Pierce Betsy S, Jiangli Yan, Katherine L. Lee, Lih-Ling Lin, Chulho Choi
Publikováno v:
Journal of Medicinal Chemistry. 60:5521-5542
Through fragment-based drug design focused on engaging the active site of IRAK4 and leveraging three-dimensional topology in a ligand-efficient manner, a micromolar hit identified from a screen of a Pfizer fragment library was optimized to afford IRA
Autor:
Michael David Rogers, Jeffery N. Carroll, Mark A. Massa, Jeffrey Hitchcock, Peter G. Ruminski, Michelle A. Schmidt, Bruce C. Hamper, Strohbach Joseph Walter, Huey S. Shieh, Laurence O. Whiteley, Katherine E. Palmquist, Joe T. Collins, Grace E. Munie, Hanau Cathleen E, H. Peter Kleine, Mark E. Schnute, T. Sunyer, Nicole Caspers, John E. Baldus, Theresa R. Fletcher, Joseph J. McDonald, Silvia Portolan, Jeffrey A. Scholten, Dean Messing, Margaret L. Grapperhaus, Brandon Collins
Publikováno v:
Journal of Medicinal Chemistry. 59:313-327
Matrix metalloproteinase-13 (MMP-13) is a zinc-dependent protease responsible for the cleavage of type II collagen, the major structural protein of articular cartilage. Degradation of this cartilage matrix leads to the development of osteoarthritis.
A practical and stereoselective synthesis of (+/−)-trans-4-benzyloctahydropyrrolo[3,4-b][1,4]oxazine
Publikováno v:
Journal of Heterocyclic Chemistry. 47:1095-1103
Starting from commercially available cis-epoxysuccinic acid (I) a facile stereoselective synthesis of title compound (V) is described.
Autor:
Jeffery A. Moeslein, William E. Mcghee, Roberta Louise Dorow, Paul M. Herrinton, Michael F. Veley, Strohbach Joseph Walter, Richard A. Hohler, Michael A. Mauragis, Mark T. Maloney
Publikováno v:
Organic Process Research & Development. 10:493-499
An efficient synthesis of N-(4-chlorobenzyl)-2-(2-hydroxyethyl)-8-(morpholin-4-ylmethyl)-6-oxo-6H-pyrrol[3.2.1-ij]quinoline-5-carboxamide (5) was developed. The route was chosen due to its reasonab...
Publikováno v:
Biopolymers. 51:51-58
Efforts to develop therapeutically relevant HIV protease inhibitors as medicinal agents in confronting the AIDS crisis have been aided by the wealth of fundamental information acquired during related drug discovery campaigns against other aspartyl pr
Autor:
Lester A. Dolak, Johnson Paul D, Chong Kt, Harvey Irving Skulnick, Paul K. Tomich, Michael John Bohanon, Strohbach Joseph Walter, Suvit Thaisrivongs, Steve Turner, K. D. Watenpaugh, M.‐M. Horng, M.N. Janakiraman, R. R. Hinshaw, Paul A. Aristoff, J. C. Lynn, Eric P. Seest, Tommasi Ruben A
Publikováno v:
Journal of Medicinal Chemistry. 41:3467-3476
A broad screening program previously identified phenprocoumon (1) as a small molecule template for inhibition of HIV protease. Subsequent modification of this lead through iterative cycles of structure-based design led to the activity enhancements of
Autor:
Suvit Thaisrivongs, Tommasi Ruben A, Chong Kt, K. D. Watenpaugh, Paul K. Tomich, Strohbach Joseph Walter, Steve R. Turner, M.N. Janakiraman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:1237-1242
Potent, non-peptidic, dihydropyrone sulfonamide HIV protease inhibitors have been previously described. Crystallographic analysis of dihydropyrone sulfonamide inhibitor/HIV protease complexes suggested incorporation of a second, C2 symmetry-related s