Výsledky vyhledávání - "Emile Johann Velthuisen"

The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors

Autor: Susan Danehower, David Temelkoff, Emile Johann Velthuisen, Kevin W. Brown, Brian A. Johns

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

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Allosteric Inhibition of Human Immunodeficiency Virus Integrase

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

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Structural Basis for Inhibitor-Induced Aggregation of HIV Integrase

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)

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

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Pyridopyrimidinone inhibitors of HIV-1 RNase H

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

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HIV Integrase Inhibitors

Autor: Takashi Kawasuji, Emile Johann Velthuisen, Brian A. Johns

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