Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Cheng-Kon Shih"'
Autor:
Steven Kerr, Charles L. Cywin, Frank H. Büttner, Frank Wu, Mohammed A. Kashem, Scott Jakes, Zofia Paw, Roger J. Snow, Erick R. R. Young, Eugene R. Hickey, Stanley Kugler, Paul Kaplita, Cheng-Kon Shih, Rhonda Chen, Anthony S. Prokopowicz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3235-3239
Two closely related scaffolds were identified through an uHTS campaign as desirable starting points for the development of Rho-Kinase (ROCK) inhibitors. Here, we describe our hit-to-lead evaluation process which culminated in the rapid discovery of p
Autor:
Peter M. Grob, Janice R. Brickwood, Cheng-Kon Shih, Maryann Hoermann, Julian Adams, Racheline Schwartz, Daniel Pauletti, Eva David, David A. Erickson, Kevin Barringer, Charles L. Cywin, David Joseph, Susan E. Hattox, Janice M. Klunder, Christopher L. Sorge
Publikováno v:
Journal of Medicinal Chemistry. 41:2960-2971
Like other nonnucleoside inhibitors of HIV-1 reverse transcriptase, the dipyridodiazepinone nevirapine (Viramune, 1) selects for drug resistant variants of HIV-1, both in cell culture and in patients. In particular, the mutation of residue 181 from t
Autor:
David D. Ho, Yunzhen Cao, Joseph W. Pav, Julian Adams, Elizabeth Muchmore, Steve Norris, Peter M. Grob, Cheng-Kon Shih
Publikováno v:
Nature Medicine. 3:665-670
Chimpanzees were challenged with HIV-1IIIB while receiving a short regimen of nevirapine (Viramune), a nonnucleoside inhibitor of HIV-1 reverse transcriptase. The untreated, control chimpanzee developed an infection characterized by seroconversion, v
Publikováno v:
Antimicrobial Agents and Chemotherapy. 38:388-391
Reverse transcriptase from feline immunodeficiency virus (FIV) has been cloned and expressed in Escherichia coli. We have purified this recombinant enzyme and shown that it is a 66-kDa protein that is indistinguishable from virion-derived FIV reverse
Autor:
Daniel J. Greenwood, Cheng-Kon Shih, Thomas C. Warren, G Piras, D Richman, Christine A. Grygon, R C Cousins, Janice M. Rose, Albino Bacolla, Richard H. Ingraham
Publikováno v:
Journal of Biological Chemistry. 268:16571-16577
Nevirapine is a highly potent and specific inhibitor of human immunodeficiency virus type 1 (HIV-1) polymerase, but is inactive against HIV-2 and other polymerase. Previous studies demonstrated that residues 176-190 of HIV-1 reverse transcriptase (RT
Autor:
Charles L. Cywin, Mohammed A. Kashem, Paul Kaplita, Wang Mao, Frank H. Büttner, Erick R. R. Young, Scott Jakes, Steven Kerr, Eugene R. Hickey, Frank Wu, Georg Dahmann, Daniel Richard Marshall, Cheng-Kon Shih, Stanley Kugler, Tina Morwick, Zofia Paw
Publikováno v:
Journal of medicinal chemistry. 53(2)
A highly selective series of bisbenzamide inhibitors of Rho-associated coiled-coil forming protein kinase (ROCK) and a related ureidobenzamide series, both identified by high throughput screening (HTS), are described. Details of the hit validation an
Publikováno v:
Molecular and Cellular Biology. 10:3397-3404
A wild-type haploid yeast strain was transformed with a library of wild-type yeast DNA fragments ligated into a high-copy-number plasmid vector (YEp24). The pooled URA+ transformants were plated on rich medium containing a lethal concentration of tri
Autor:
Gerald Nabozny, Zofia Paw, Laura Beck, Daniel Kuzmich, Alison Kukulka, Richard M. Nelson, John R. Proudfoot, David S. Thomson, Younes Bekkali, Mario G. Cardozo, Cheng-Kon Shih, Patty Reilly, Rodney P. DeLeon, Kirrane Thomas M, Renee Zindell
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(18)
A new series of ligands for the glucocorticoid receptor (GR) is described. SAR development was guided by docking 3 into the GR active site and optimizing an unsubstituted phenyl ring for key interactions found in the steroid A-ring binding pocket. To
Autor:
Daniel Kuzmich, Yan Zhang, Jörg Bentzien, Mario G. Cardozo, Raj Betageri, Alison Capolino, Richard M. Nelson, Gerald Nabozny, Zofia Paw, Renee Zindell, Daw-Tsun Shih, Cheng-Kon Shih, David S. Thomson, Ljiljana Zuvela-Jelaska, Kirrane Thomas M, Tazmeen N. Fadra
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(21)
Compound 1, a potent glucocorticoid receptor ligand, contains a quaternary carbon bearing trifluoromethyl and hydroxyl groups. This paper describes the effect of replacing the trifluoromethyl group on binding and agonist activity of the GR ligand 1.
Autor:
Peter M. Grob, Richard H. Ingraham, Tari L. Mctague, Cheng-Kon Shih, Vincent J. Merluzzi, Joe C. Wu, Karl D. Hargrave, Kenneth A. Cohen
Publikováno v:
AIDS research and human retroviruses. 8(2)
Nevirapine, a dipyridodiazepinone, is a highly specific inhibitor of HIV-1 reverse transcriptase (RT) which exhibits an IC50 = 84nM in enzyme assays and IC50 = 40nM against HIV-1 replication in cell culture. This nonnucleoside inhibitor acts noncompe