Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Rosemarie Sellati"'
Autor:
Rosemarie Sellati, Jianfei Yang, Tin Min Htut, Xiang Li, Adedayo Hanidu, Lian Wang, Huiping Jiang, Jun Li
Publikováno v:
Immunology. 131:174-182
PIM (proviral integration site) kinases are a distinct class of serine/threonine-specific kinases consisting of PIM1, PIM2 and PIM3. PIM2 is known to function in apoptosis pathways. Expression of PIM2 is highly induced by pro-inflammatory stimuli but
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
Autor:
Rosemarie Sellati, Huiping Jiang, Melissa A. Pegues, Mary McFarland, Lynn Pantages, Jeffrey B. Madwed, Rajvee Parikh, Steven Kerr, Jorge Villalona, Alexander J. Szalai, Valentina Berger, Nicholas R. Jones, Mark A. McCrory
Publikováno v:
Arthritis and rheumatism. 63(9)
Blood C-reactive protein (CRP) is routinely measured to gauge inflammation. In rheumatoid arthritis (RA), a heightened CRP level is predictive of a poor outcome, while a lowered CRP level is indicative of a positive response to therapy. CRP interacts
Autor:
Jianfei, Yang, Xiang, Li, Adedayo, Hanidu, Tin M, Htut, Rosemarie, Sellati, Lian, Wang, Huiping, Jiang, Jun, Li
Publikováno v:
Immunology. 131(2)
PIM (proviral integration site) kinases are a distinct class of serine/threonine-specific kinases consisting of PIM1, PIM2 and PIM3. PIM2 is known to function in apoptosis pathways. Expression of PIM2 is highly induced by pro-inflammatory stimuli but
Autor:
Stanley Kugler, Mohammed A. Kashem, Ernest L. Raymond, Hidenori Takahashi, Steven S. Pullen, Leslie Martin, Gabriel Labissiere, Jennifer Ahlberg, Jennifer A. Kowalski, Hnin Hnin Khine, Joseph R. Woska, Stéphane De Lombaert, Donna Skow, David S. Thomson, Kathy O’Shea, Brian Nicholas Cook, Renee Zindell, Deborah D. Jeanfavre, Doris Riether, Jörg Bentzien, Kerry L. M. Ralph, Rosemarie Sellati
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(6)
Benzamide 1 demonstrated good potency as a selective ITK inhibitor, however the amide moiety was found to be hydrolytically labile in vivo, resulting in low oral exposure and the generation of mutagenic aromatic amine metabolites. Replacing the benza
Autor:
Michael P. Winters, Renee L. DesJarlais, Paul Kaplita, Hnin Hnin Khine, Kevin J. Moriarty, Steven S. Pullen, Ernest L. Raymond, Roger J. Snow, Rosemarie Sellati, Gregory P. Roth, Charles L. Cywin, Thomas M. Farrell, Lisa H. Liu, Mohammed A. Kashem, Hidenori Takahashi, Darius Robinson, Joseph R. Woska, Josephine King, John P. Wolak
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(20)
A series of novel 5-aminomethyl-1H-benzimidazole based inhibitors of Itk were prepared. Structure–activity relationships, selectivity and cell activity are reported for this series. Compound 2, a potent and selective antagonist of Itk, inhibited an
Autor:
Jie Zhao, Tin Min Htut, Xinshou Ouyang, Hongxing Li, Adedayo Hanidu, Rosemarie Sellati, Jay C. Unkeless, Jun Li, Shu Zhang, Jianfei Yang, Huabao Xiong, Xiang Li, Adrian T. Ting, Mark E. Labadia, Martin Hodge, Huiping Jiang, Min Yang, Lloyd Mayer
Publikováno v:
European journal of immunology. 38(5)
Epstein-Barr virus-induced gene 3 (EBI3) associates with p28 to form IL-27 and with IL-12p35 to form IL-35. IL-27Ralpha(-/-) mice studies indicate that IL-27 negatively regulates Th17 cell differentiation. However, no EBI3, p28 or p35-deficiency stud
Autor:
David Joseph, Y.-C. Tseng, Amy Gao, Jiang-Ping Wu, R. Wasti, Daniel R. Goldberg, Ming-Hong Hao, Younggi Choi, Chris Pargellis, Mohammed A. Kashem, Zhaoming Xiong, Derek Cogan, Brian Werneburg, Matthew R. Netherton, Rosemarie Sellati, Ji Wang, Carol A. Torcellini, Josephine Pelletier, Donna Skow, Rodney P. DeLeon, Miller Craig Andrew, Lore Gruenbaum, M. Corson, Neil Moss
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(3)
Optimization of pyrazinoindolone inhibitors of MAPKAP-K2 (MK2) provides a reasonable balance of cellular potency and physicochemical properties. Mechanistic studies support the inhibition of MK2 which is responsible for the sub-micromolar cellular ef
Autor:
Ian Potocki, Shirlynn Chen, Rosemarie Sellati, Patricia L. Reilly, Kei Kishimoto, Emeigh Jonathan Emilian, Gerald Nabozny, Robert Rothlein, Donghong A. Gao, Miao Clara K, Daniel R. Goldberg, Sorcek Ronald J, Daniel Kuzmich, Terence A. Kelly, Drané O'Brien, Deborah D. Jeanfavre, Charline Peng, and Stephen H. Norris, Kevin Chungeng Qian, Elizabeth Mainolfi, Wu Jiang-Ping, Joseph R. Woska, Jocelyn A. Gunn
Publikováno v:
Journal of medicinal chemistry. 47(22)
A novel class of lymphocyte function-associated antigen-1 (LFA-1) inhibitors is described. Discovered during the process to improve the physicochemical and metabolic properties of BIRT377 (1, Figure 1), a previously reported hydantoin-based LFA-1 inh
Autor:
Yong Wang, Anthony S. Prokopowicz, Suresh R. Kapadia, Matt Aaron Tschantz, Maret Panzenbeck, Jonathan Tan, Pla Xiong, John P. Wolak, Xiao-Jun Wang, Susan Pav, Susan Lukas, Scott Jakes, Tina Morwick, Mario G. Cardozo, Usha R. Patel, Tanja Butz, Gregory W. Peet, Hidenori Takahashi, Neil Moss, Robert J. Eckner, Jeffrey D. Peterson, Abdelhakim Hammach, Mohammed A. Kashem, Daniel R. Goldberg, Jessica Huang, Roger J. Snow, Rosemarie Sellati
Publikováno v:
Journal of medicinal chemistry. 46(8)
The tyrosine kinase p56lck (lck) is essential for T cell activation; thus, inhibitors of lck have potential utility as autoimmune agents. Our initial disclosure of a new class of lck inhibitors based on the phenylaminoimidazoisoquinolin-9-one showed