Zobrazeno 1 - 10 of 17 pro vyhledávání: '"Peter M. Grob"'
1
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site
Autor: Pier F. Cirillo, Susan Pav, John R. Regan, L. Churchill, Eugene R. Hickey, A. G. Graham, Liang Tong, Gilmore Thomas A, Neil Moss, Peter M. Grob, Christopher Pargellis
Publikováno v: Nature Structural Biology. 9:268-272
The p38 MAP kinase plays a crucial role in regulating the production of proinflammatory cytokines, such as tumor necrosis factor and interleukin-1. Blocking this kinase may offer an effective therapy for treating many inflammatory diseases. Here we r
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c77f6b3730f55d45d9031499877f5a5
https://doi.org/10.1038/nsb770
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2
Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 7. 8-Arylethyldipyridodiazepinones as Potent Broad-Spectrum Inhibitors of Wild-Type and Mutant Enzymes
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
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::469f46d7150995a5240574cb8a29e512
https://doi.org/10.1021/jm9707028
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3
Prophylaxis against HIV-1 infection in chimpanzees by nevirapine, a nonnucleoside inhibitor of reverse transcriptase
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
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72c515d4fa441209b9a38003b9a4448b
https://doi.org/10.1038/nm0697-665
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4
Selective inhibition of human cyclo-oxygenase-2 by meloxicam
Autor: L. Churchill, Peter M. Grob, D. Pauletti, C-K. Shih, Peter R. Farina, A. G. Graham
Publikováno v: InflammoPharmacology. 4:125-135
Human cyclo-oxygenase-1 (hCOX-1) and-2 were expressed in stable transfected COS A.2 cells and in insect cells using a Sf9 baculovirus expression system. Inhibition of COX activity was examined using both whole cell and microsomal assays. Ibuprofen, n
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::79226464123695b5e84b8922adf5ba2d
https://doi.org/10.1007/bf02735467
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5
Novel Non-nucleoside Inhibitors of Human Immunodeficiency Virus Type 1 Reverse Transcriptase. 5. 4-Substituted and 2,4-Disubstituted Analogs of Nevirapine
Autor: Eva David, Mcneil Daniel W, Julian Adams, John R. Proudfoot, Mario G. Cardozo, Atul Agarwal, Usha R. Patel, Karl D. Hargrave, Peter M. Grob, Terence A. Kelly
Publikováno v: Journal of Medicinal Chemistry. 38:4839-4847
Molecular modeling analysis of the recently published X-ray crystal structure of nevirapine bound to wild type human immunodeficiency virus type 1 reverse transcriptase (WT-RT) indicated the presence of a lipophilic cavity proximal to the 4-position
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c7263b79d65e48a167bba3a04d860c6
https://doi.org/10.1021/jm00024a011
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6
High-performance liquid chromatography and photoaffinity crosslinking to explore the binding environment of nevirapine to reverse transcriptase of human immunodeficiency virus type-1
Autor: Thomas C. Warren, Deborah E.H. Palladino, Peter M. Grob, Suresh R. Kapadia, Kenneth A. Cohen, Jerry L. Hopkins, Richard H. Ingraham, James M. Stevenson, Glenn J. Van Moffaert
Publikováno v: Journal of Chromatography A. 676:99-112
Nevirapine (BI-RG-587) is a potent inhibitor of the polymerase activity of reverse transcriptase of human immunodeficiency virus type-1. Nevirapine, as well as several other non-nucleoside compounds of various structural classes, bind strongly at a s
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4a0860e4e9979ad80415c6d4a6ca457e
https://doi.org/10.1016/0021-9673(94)80458-3
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8
Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity
Autor: Sorcek Ronald J, Simon J. Coutts, L. Churchill, Eva David, Mcneil Daniel W, Gunter Trummlitz, Hin-Chor Wong, Peter M. Grob, Ian Potocki, Hans Meier, Matt Aaron Tschantz, Wolfhard Engel, Lazer Edward S, Miao Clara K, A. G. Graham, Terence A. Kelly, Charles L. Cywin, Maryann Hoermann, Zhaoxing Meng, Roger J. Snow
Publikováno v: Journal of medicinal chemistry. 40(6)
Meloxicam (5), an NSAID in the enol-carboxamide class, was developed on the basis of its antiinflammatory activity and relative safety in animal models. In subsequent screening in microsomal assays using human COX-1 and COX-2, we discovered that it p
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50186f66868fad80b86b655e901a13d8
https://pubmed.ncbi.nlm.nih.gov/9083488
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9
Nonnucleoside inhibitors of HIV-1 reverse transcriptase: nevirapine as a prototype drug
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
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4d1cd1017b6b6b0b19310cb2d180c60
https://pubmed.ncbi.nlm.nih.gov/1371691
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10
Steady state kinetics and inhibition of HIV-1 reverse transcriptase by a non-nucleoside dipyridodiazepinone, BI-RG-587, using a heteropolymeric template
Autor: Peter M. Grob, Anthony Shrutkowski, John Miglietta, Mark T. Skoog, Elizabeth B. Kopp, Cheng-Kon Shih
Steady state kinetics and inhibition by a dipyridodiazepinone of the reverse transcriptase from human immunodeficiency virus type 1 (HIV) were studied using a heteropolymeric RNA template with a sequence from the authentic initiation site on the HIV
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad8394d81a07f3db529583fced7908ea
https://europepmc.org/articles/PMC328267/
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