Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Emile Johann Velthuisen"'
Publikováno v:
European Journal of Medicinal Chemistry. 117:99-112
A novel series of HIV-1 integrase strand transfer inhibitors were designed using the venerable two-metal binding pharmacophore model and incorporating structural elements from two different literature scaffolds. This manuscript describes a number of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a06644c82bc4476e5604c544b81e2660
https://doi.org/10.1016/j.ejmech.2016.03.038
https://doi.org/10.1016/j.ejmech.2016.03.038
Autor:
Troy Brady, Benjamin M. Dyer, Emile Johann Velthuisen, Nirav Malani, Kushol Gupta, Jerry Jeffrey, Gregory D. Van Duyne, Young Hwang, Liping Wang, Frances Male, Robert T. Nolte, Frederic D. Bushman
Publikováno v:
Journal of Biological Chemistry. 289:20477-20488
HIV-1 replication in the presence of antiviral agents results in evolution of drug-resistant variants, motivating the search for additional drug classes. Here we report studies of GSK1264, which was identified as a compound that disrupts the interact
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::82e64e87e11f3a4ad17bd100ffd0db46
https://doi.org/10.1074/jbc.m114.551119
https://doi.org/10.1074/jbc.m114.551119
Autor:
Robert T. Nolte, Louis J. Taylor, Scott Sherrill-Mix, Gregory D. Van Duyne, Jerry Jeffrey, Young Hwang, Charlene B. McDanal, Kushol Gupta, Grant Eilers, David Temelkoff, Ping Wang, Vesa Turkki, Emile Johann Velthuisen, Frederic D. Bushman
Publikováno v:
PLoS Biology
PLoS Biology, Vol 14, Iss 12, p e1002584 (2016)
PLoS Biology, Vol 14, Iss 12, p e1002584 (2016)
The allosteric inhibitors of integrase (termed ALLINIs) interfere with HIV replication by binding to the viral-encoded integrase (IN) protein. Surprisingly, ALLINIs interfere not with DNA integration but with viral particle assembly late during HIV r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::929c139499a2b190d4d75ed8749a29f3
http://europepmc.org/articles/PMC5147827
http://europepmc.org/articles/PMC5147827
Autor:
Brian A. Johns, Emile Johann Velthuisen, Kendra E. Hightower, John W. Seal, Peter Gerondelis, Kevin K. Brown, Ming Li, Lisa A. Leesnitzer, Wenwen Zhang, Yan Chen, Sonia R. Miranda, Ke Mou
Publikováno v:
European journal of medicinal chemistry. 83
Using a structure based pharmacophore design, a weak inhibitor of RNase H, identified from a small library of two metal binding HIV-1 integrase inhibitors, was optimized for potency and physicochemical properties. This manuscript describes the SAR an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2bd973f72221ddfffa959c04284f6b71
https://pubmed.ncbi.nlm.nih.gov/24997293
https://pubmed.ncbi.nlm.nih.gov/24997293
Publikováno v:
Successful Strategies for the Discovery of Antiviral Drugs ISBN: 9781849736572
This chapter presents the discovery, development and evolution of integrase strand transfer inhibitors. A brief overview of the first‐generation inhibitors raltegravir and elvitegravir serves to describe their landmark advancement of the field and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f26d9dc7499101dee7f61cc52926badb
https://doi.org/10.1039/9781849737814-00149
https://doi.org/10.1039/9781849737814-00149
