Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Richard E. Showalter"'
Autor:
Richard E. Showalter, Jim Thomson, Yudou He, Mario Meng-Chiang Kuo, Richard Hickey, Wei-Jong Shia, Li-Chang Chen, Elena Brin, Eleanor Dagostino, Katherine Wu, Robert Almassy, Mariusz Stempniak
Publikováno v:
Oncotarget
Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) binds to death receptors and induces apoptosis in various cancer cell lines while sparing normal cells. Recombinant TRAIL has shown good safety and efficacy profiles in preclinical
Autor:
Richard E. Showalter, Wei-Jong Shia, Jim Thomson, Elena Brin, Bob Almassy, Eleanor Dagostino, Li-Chang Chen, Richard Hickey, Mario Meng-Chiang Kuo, Katherine Wu, Yudou He
Publikováno v:
Cancer Research. 78:3902-3902
TNF-related apoptosis-inducing ligand (TRAIL) receptor agonists have shown good safety profile and efficacy in preclinical cancer models. However, clinical success has been limited due to poor PK and/or development of resistance to death receptor-ind
Autor:
Laurie A. LeBrun, Mei Tsan, Yuefen Zhou, Frank Ruebsam, Darian M. Bartkowski, Alan X. Xiang, Ruhi Kamran, Lian-Sheng Li, Richard E. Showalter, Jingjing Zhao, Rupal Patel, Matthew Lardy, Maria V. Sergeeva, Stephen E. Webber, Amit M. Shah, David Archer Ellis, Zhongxiang Sun, Mcguire Helen, Julie Blazel, Leo Kirkovsky, Daniel A. Norris, Tran Chinh Viet, Charles R. Kissinger, Thomas G. Nolan, Peter S. Dragovich, Qing Han
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4628-4632
4-(1,1-Dioxo-1,4-dihydro-1lambda(6)-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-one analogs were discovered as a novel class of inhibitors of HCV NS5B polymerase. Structure-based design led to the identification of compound 3a that displayed pot
Autor:
Tran Chinh Viet, Charles R. Kissinger, Daniel A. Norris, Ruhi Kamran, Amit M. Shah, Jingjing Zhao, Yuefen Zhou, Rupal Patel, Matthew Lardy, Darian M. Bartkowski, Richard E. Showalter, Stephen E. Webber, Laurie A. LeBrun, Mei Tsan, Douglas E. Murphy, Sun Hee Kim, Maria V. Sergeeva, Leo Kirkovsky, Martin T. Tran, Thomas G. Nolan, Qing Han, Frank Ruebsam, Lian-Sheng Li, Peter S. Dragovich
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3616-3621
Pyrrolo[1,2-b]pyridazin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Structure-based design led to the discovery of compound 3 k, which displayed potent inhibitory activities in biochemical and repli
Autor:
Bin Li, Lindsay J. Howett, Shaohui Wang, Rupal Patel, Richard E. Showalter, Mei-Mei Wang, April Averill, Peggy A. Thompson, James R. Appleman
Publikováno v:
ASSAY and Drug Development Technologies. 6:69-81
ATLAS (Any Target Ligand Affinity Screen) (Anadys Pharmaceuticals, Inc., San Diego, CA) is a homogeneous, affinity-based high-throughput screening technology based on protein thermal denaturation and the ability of ligands to bind and stabilize the t
Autor:
Tran Chinh Viet, Douglas E. Murphy, Stephen E. Webber, Bin Li, Thomas Hermann, Zhongxiang Sun, Charles R. Kissinger, Rupal Patel, Frank Ruebsam, Maria V. Sergeeva, Peter S. Dragovich, Lian-Sheng Li, Yuefen Zhou, Richard E. Showalter, Amit M. Shah, Laurie A. LeBrun, Qing Han, Qiang Zhao, Leo Kirkovsky, Mei Tsan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1413-1418
5-Hydroxy-3(2H)-pyridazinone derivatives were investigated as inhibitors of genotype 1 HCV NS5B polymerase. The synthesis, structure–activity relationships (SAR), metabolic stability, and structure-based design approach for this new class of compou
Autor:
Yuefen Zhou, Frank Ruebsam, Richard E. Showalter, Thomas Hermann, Lian-Sheng Li, Rupal Patel, Mei Tsan, April Averill, Qiang Zhao, Douglas E. Murphy, Qing Han, Peter S. Dragovich, Charles R. Kissinger, Laurie A. LeBrun, Maria V. Sergeeva, Amit M. Shah, Stephen E. Webber, Tran Chinh Viet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1419-1424
5-Hydroxy-3(2H)-pyridazinone derivatives were investigated as inhibitors of genotype 1 HCV NS5B polymerase. The structure-activity relationship (SAR) associated with variation of the pyridazinone 2- and 6-substituents is discussed. The synthesis and
Autor:
Stephen E. Webber, Amit M. Shah, Kevin R. Steffy, James R. Appleman, Alan X. Xiang, Robert M. Aust, Thomas Doundoulakis, Richard E. Showalter, Klaus B. Simonsen, William T. Biller, Virginia N. Banh, Wes Sisson, Ricardo Lira, Konstantinos A. Agrios
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6797-6800
Based upon observations from our initial findings, additional myxopyronin B analogs have been prepared and tested for in vitro inhibitory activity against DNA-dependent RNA polymerase and antibacterial activity against Escherichia coli and Staphyloco
Autor:
Dong Liming, Xinjun Hou, Elizabeth A. Lunney, Corinne E. Augelli-Szafran, Deal Judith G, Christopher F. Bigge, Darin Vanderpool, Raymond Andrew Hudack, Nancy Sue Barta, Bradley William Caprathe, Chuangxing Guo, Steve Bender, Richard E. Showalter, Lorraine Kathleen Fay, Arindam Chatterjee
Publikováno v:
Journal of Medicinal Chemistry. 49:1202-1206
Since the discovery that FK-506 promotes neurite outgrowth, considerable attention has been focused on the development of potent nonimmunosuppressive ligands for FK-506 binding proteins (FKBPs). Such neuroimmunophilin agents have been reported to sho
Autor:
Michele Ann Mctigue, Michael R Gehring, Chris Pinko, J. Ernest Villafranca, Chen-Chen Kan, Camran V Parast, Krzysztof Appelt, Richard E. Showalter, Barbara Mroczkowski, John A Wickersham, Anna Tempczyk-Russell
Publikováno v:
Structure. 7:319-330
Background: Angiogenesis is involved in tumor growth, macular degeneration, retinopathy and other diseases. Vascular endothelial growth factor (VEGF) stimulates angiogenesis by binding to specific receptors (VEGFRs) on the surface of vascular endothe