Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Eva, Papp"'
Autor:
Mcintosh Joel, Andreas Kuglstatter, Paul Weller, Sarah C. Abbot, David C. Swinney, Brad Loe, Tobias Gabriel, Roland J. Billedeau, Martin Stahl, Hasim Zecic, Nidhi Arora, Eva Papp, Humberto Bartolome Arzeno, Brian Wong, Allassan Abubakari, Nolan James Dewdney, David Michael Goldstein, Man-Ling Sung, Rebecca T Suttman, Michael Soth, Jaehyeon Park, Kieran Durkin, Fujun Li, Manjiri Ghate, Kristen Lynn Mccaleb, Sandra Frauchiger, Ronald J. Hill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3452-3456
Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile.
Autor:
Jaehyeon Park, Harlan F Reese, Yun-Chou Tan, Hasim Zecic, Martin Stahl, Keshab Sarma, Renee Litman, Alejandra Trejo, William Bingenheimer, Michael Soth, David Michael Goldstein, Mary Welch, Eric Brian Sjogren, Man-Ling Sung, Sandra Frauchiger, Nolan James Dewdney, Bong San Pablo, Eva Papp, Daniel McWeeney, Ronald J. Hill, Paul Weller, Manjiri Ghate, JoAnn La Fargue, Brian Wong, Stacie A. Dalrymple, James Patrick Dunn, David Mark Rotstein, Richard T. Roberts, Bradford Graves, Rebecca T Suttman, Mcintosh Joel, Farrell Robert P, Andreas Kuglstatter, Chen Jian Jeffrey, Fujun Li, Humberto Bartolome Arzeno, Brad Loe, Tobias Gabriel
Publikováno v:
Journal of Medicinal Chemistry. 54:2255-2265
The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently in
Publikováno v:
Analytical Biochemistry. 395:256-262
Novel biochemical strategies are needed to identify the next generation of protein kinase inhibitors. One promising new assay format is a competition binding approach that employs time-resolved fluorescence resonance energy transfer (TR–FRET). In t
Autor:
Emily Tsang, Shaan Gandhi, David E. Shaw, Marie Dinh, J. Michael Bradshaw, Eva Papp, Joyce K. Y. Tse, Anthony M. Giannetti, Sandra Wang, Hoangdung Ho
Publikováno v:
Journal of Biological Chemistry. 283:32650-32659
Many immune signaling pathways require activation of the Syk tyrosine kinase to link ligation of surface receptors to changes in gene expression. Despite the central role of Syk in these pathways, the Syk activation process remains poorly understood.
Autor:
Yong-Nam Kim, Stanford L. Peng, Anthony M. Manning, Joseph Dal Porto, Karim Dabbagh, Ronald J. Hill, Mary Welch, Kyung Song, Tanja S. Zabka, Ching Li, Dee Aud, Rebecca Suttmann, David Leaffer, Kung-ching Chang, Eva Papp, Brian Wong, Deborah Phippard, David Michael Goldstein, Richard T. Roberts
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 327:610-619
P38alpha is a protein kinase that regulates the expression of inflammatory cytokines, suggesting a role in the pathogenesis of diseases such as rheumatoid arthritis (RA) or systemic lupus erythematosus. Here, we describe the preclinical pharmacology
Autor:
Jim Barnett, Eva Papp, David C. Swinney, J. Michael Bradshaw, Joyce K. Y. Tse, Hoangdung Ho, Sandra Wang, David E. Shaw, Simon Lee
Publikováno v:
Biochemistry. 46:15103-15114
Spleen tyrosine kinase (Syk) is a cytoplasmic tyrosine kinase that plays an important signaling role in several types of immune cells. To improve our understanding of the enzymology and activation mechanism of Syk, we characterized the steady state k
Autor:
Han-Zhong Zhang, Eva Papp, John C. Wu, Kotesvar Rao, Kenneth Straub, Stephen F. Carr, Josef Fried
Publikováno v:
Journal of Medicinal Chemistry. 40:4-8
Functionalized 2-alkyl derivatives of inosinic acid have been synthesized to serve as reversible as well as irreversible inhibitors of the human type II enzyme inosine monophosphate dehydrogenase. These compounds were designed to react with Cys-331 o
Autor:
Carlos Gonzalez, Stephen F. Carr, Elsie M. Eugui, Rebecca A. Stephenson, Fidencio Franco, Peter H. Nelson, Ann-Marie Waltos, Eric Brian Sjogren, Sussan Rouhafza, Francisco Xavier Talamas, Ronald Charles Hawley, Devens Bruce H, David G. Loughhead, Robert James Weikert, Patterson John W, Eva Papp, David J. Milan, John C. Wu, David Bernard Smith
Publikováno v:
Journal of Medicinal Chemistry. 39:4181-4196
Structure-activity relationships in the region of the phthalide ring of the inosine monophosphate dehydrogenase inhibitor mycophenolic acid have been explored. Replacement of the lactone ring with other cyclic moieties resulted in loss of potency, es
Autor:
David M, Goldstein, Michael, Soth, Tobias, Gabriel, Nolan, Dewdney, Andreas, Kuglstatter, Humberto, Arzeno, Jeffrey, Chen, William, Bingenheimer, Stacie A, Dalrymple, James, Dunn, Robert, Farrell, Sandra, Frauchiger, JoAnn, La Fargue, Manjiri, Ghate, Bradford, Graves, Ronald J, Hill, Fujun, Li, Renee, Litman, Brad, Loe, Joel, McIntosh, Daniel, McWeeney, Eva, Papp, Jaehyeon, Park, Harlan F, Reese, Richard T, Roberts, David, Rotstein, Bong, San Pablo, Keshab, Sarma, Martin, Stahl, Man-Ling, Sung, Rebecca T, Suttman, Eric B, Sjogren, Yunchou, Tan, Alejandra, Trejo, Mary, Welch, Paul, Weller, Brian R, Wong, Hasim, Zecic
Publikováno v:
Journal of medicinal chemistry. 54(7)
The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently in
Publikováno v:
Planta Medica. 77