Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Charles R. Kissinger"'
Publikováno v:
Frontiers in Neurology, Vol 13 (2022)
Background and purposeJ147, a novel neurotrophic compound, was originally developed to treat aging-associated neurological diseases. Based on the broad spectrum of cytoprotective effects exhibited by this compound, we investigated whether J147 has ce
Externí odkaz:
https://doaj.org/article/b67bb812dc3143ec975ffd388d15fc3c
Publikováno v:
Journal of Chemical Information and Modeling. 52:1328-1336
In modern day drug discovery campaigns, computational chemists have to be concerned not only about improving the potency of molecules but also reducing any off-target ADMET activity. There are a plethora of antitargets that computational chemists may
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:
Masaki Tomimoto, Stephanie Hopkins, Brian E. Nolan, Jeff Blaney, Anthony M. Giannetti, Seth F. Harris, Michelle F. Browner, Normand Hebert, Jorg Hendle, Eduardo Torres, Brandon E. Aubol, Ethel McGee, David Marciano, Tobi A Wright, Isabel Najera, Elizabeth A. Jefferson, Charles R. Kissinger, Vincent Leveque, Stephen Suresh Antonysamy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2990-2995
Non-nucleoside inhibitors of HCV NS5b RNA polymerase were discovered by a fragment-based lead discovery approach, beginning with crystallographic fragment screening. The NS5b binding affinity and biochemical activity of fragment hits and inhibitors w
Publikováno v:
Acta Crystallographica Section D Biological Crystallography. 64:436-443
The hepatitis C (HCV) internal ribosome entry site (IRES) element plays a central role in cap-independent translation of the viral genomic RNA. The unique conformation of IRES domain II is critical for 80S ribosomal assembly and initiation of viral t
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:
A.Keith Dunker, J.David Lawson, Celeste J Brown, Ryan M Williams, Pedro Romero, Jeong S Oh, Christopher J Oldfield, Andrew M Campen, Catherine M Ratliff, Kerry W Hipps, Juan Ausio, Mark S Nissen, Raymond Reeves, ChulHee Kang, Charles R Kissinger, Robert W Bailey, Michael D Griswold, Wah Chiu, Ethan C Garner, Zoran Obradovic
Publikováno v:
Journal of Molecular Graphics and Modelling. 19:26-59
Proteins can exist in a trinity of structures: the ordered state, the molten globule, and the random coil. The five following examples suggest that native protein structure can correspond to any of the three states (not just the ordered state) and th
Autor:
L. A. K. Pelletier, John H. Tatlock, Xinjun J. Hou, Richard E. Showalter, M. Angelica Linton, J. Ernest Villafranca, Charles R. Kissinger, Anna Tempczyk
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:1007-1012
The design, synthesis, and evaluation of small molecule, in vitro, inhibitors of human calcineurin is described. These ligands were derived from the known nonspecific phosphatase inhibitor endothall, and were modified to enhance binding and selectivi
Autor:
A.K. Ganguly, Taveras Arthur G, Robert M. Aust, Doll Ronald J, Mark E. Snow, W. Sisson, Birendra N. Pramanik, D. M. Delisle, Charles R. Kissinger, Shella A. Fuhrman, Mary M. Senior, Bancha Vibulbhan, Yu-Sen Wang, C.A. Evans, Paul Kirschmeier, Stacy W. Remiszewski, B.B. Bauer, Louise M. Perkins, V. Girijavallabhan, D. Cesarz, Robert A. Love, Joseph J. Catino, Eric C. Huang, C. Nash, Joan E. Brown, Larry Heimark, Donna Carr, Linda James, E. Villafranca, Anthony Tsarbopoulos, Edward L. Brown, S.E. Webber, Thomas F. Hendrickson, Stephen D. Liberles, J. del Rosario
Publikováno v:
Bioorganic & Medicinal Chemistry. 5:125-133
The nucleotide exchange process is one of the key activation steps regulating the ras protein. This report describes the development of potent, non-nucleotide, small organic inhibitors of the ras nucleotide exchange process. These inhibitors bind to