Results 31 to 40 of about 2,882,240 (203)

Comparative biochemical analysis of HIV-1 subtype B and C integrase enzymes

Retrovirology, 2009
Background Integrase inhibitors are currently being incorporated into highly active antiretroviral therapy (HAART). Due to high HIV variability, integrase inhibitor efficacy must be evaluated against a range of integrase enzymes from different subtypes ...
Kuhl Björn D, Donahue Daniel A, Faltenbacher Verena H, Sloan Richard D, Bar-Magen Tamara, Oliveira Maureen, Xu Hongtao, Wainberg Mark A   +7 more
doaj   +1 more source

Structure-Guided Optimization of HIV Integrase Strand Transfer Inhibitors [PDF]

Journal of Medicinal Chemistry, 2017
Integrase mutations can reduce the effectiveness of the first-generation FDA-approved integrase strand transfer inhibitors (INSTIs), raltegravir (RAL) and elvitegravir (EVG). The second-generation agent, dolutegravir (DTG), has enjoyed considerable clinical success; however, resistance-causing mutations that diminish the efficacy of DTG have appeared ...
Zhao, Xue Zhi, Smith, Steven, Maskell, Daniel, Métifiot, Mathieu, Pye, Valerie, Fesen, Katherine, Marchand, Christophe, Pommier, Yves, Cherepanov, Peter, Hughes, Stephen, Burke, Terrence   +10 more
openaire   +3 more sources

Surveillance of HIV-1 transmitted integrase strand transfer inhibitor resistance in the UK. [PDF]

J Antimicrob Chemother, 2020
BACKGROUND:HIV treatment guidelines have traditionally recommended that all HIV-positive individuals are tested for evidence of drug resistance prior to starting ART.
Mbisa JL, Ledesma J, Kirwan P, Bibby DF, Manso C, Skingsley A, Murphy G, Brown A, Dunn DT, Delpech V, Geretti AM.   +10 more
europepmc   +3 more sources

The strand transfer oligonucleotide inhibitors of HIV-integrase

Journal of Enzyme Inhibition and Medicinal Chemistry, 2008
Retroviral integrase participates in two catalytic reactions, which require interactions with the two ends of the viral DNA in the 3'processing reaction, and with a targeted host DNA in the strand transfer reaction. The 3'-hydroxyl group of 2'-deoxyadenosine resulting from the specific removing of GT dinucleotide from the viral DNA in the processing ...
Jan, Snásel, Ivan, Rosenberg, Ondrej, Paces, Iva, Pichová   +3 more
openaire   +2 more sources

Integrase-deficient lentiviral vectors mediate efficient gene transfer to human vascular smooth muscle cells with minimal genotoxic risk [PDF]

, 2012
We have previously shown that injury-induced neointima formation was rescued by adenoviral-Nogo-B gene delivery. Integrase-competent lentiviral vectors (ICLV) are efficient at gene delivery to vascular cells but present a risk of insertional mutagenesis.
Sessa, W.C., Chick, H.E., Kane, N.M., Baker, A.H., Thrasher, A.J., Alba, R., Fronza, R., McDonald, R.A., Delles, C., Schmidt, M., Nowrouzi, A.   +10 more
core   +1 more source

Multiple choices for HIV therapy with integrase strand transfer inhibitors [PDF]

Retrovirology, 2012
Two integrases inhibitors, raltegravir and elvitegravir, have now been approved by regulatory agencies for use in the treatment of HIV-infected patients; and the approval of a third such drug, dolutegravir, is expected during 2013 on the basis of several phase 3 clinical trials.
Raffi Francois, Wainberg Mark A
openaire   +3 more sources

Structure of a HIV-1 IN-Allosteric inhibitor complex at 2.93 Å resolution: Routes to inhibitor optimization.

PLoS Pathogens, 2023
HIV integrase (IN) inserts viral DNA into the host genome and is the target of the strand transfer inhibitors (STIs), a class of small molecules currently in clinical use.
Grant Eilers, Kushol Gupta, Audrey Allen, Saira Montermoso, Hemma Murali, Robert Sharp, Young Hwang, Frederic D Bushman, Gregory Van Duyne   +8 more
doaj   +1 more source

Novel therapeutic strategies targeting HIV integrase

BMC Medicine, 2012
Integration of the viral genome into host cell chromatin is a pivotal and unique step in the replication cycle of retroviruses, including HIV. Inhibiting HIV replication by specifically blocking the viral integrase enzyme that mediates this step is an ...
Quashie Peter K, Sloan Richard D, Wainberg Mark A   +2 more
doaj   +1 more source

Three main mutational pathways in HIV-2 lead to high-level raltegravir and elvitegravir resistance: implications for emerging HIV-2 treatment regimens. [PDF]

PLoS ONE, 2012
Human immunodeficiency virus type 2 (HIV-2) is intrinsically resistant to non-nucleoside reverse transcriptase inhibitors and exhibits reduced susceptibility to several of the protease inhibitors used for antiretroviral therapy of HIV-1. Thus, there is a
Robert A Smith, Dana N Raugi, Charlotte Pan, Matthew Coyne, Alexandra Hernandez, Brad Church, Kara Parker, James I Mullins, Papa Salif Sow, Geoffrey S Gottlieb, University of Washington-Dakar HIV-2 Study Group   +10 more
doaj   +1 more source

Integrase Strand Transfer Inhibitor-Related Changes in Body Mass Index and Risk of Diabetes: A Prospective Study From the RESPOND Cohort Consortium. [PDF]

Clin Infect Dis
BACKGROUND With integrase strand transfer inhibitor (INSTI) use associated with increased body mass index (BMI) and BMI increases associated with higher diabetes mellitus (DM) risk, this study explored the relationship between INSTI/non-INSTI regimens,
Rupasinghe D, Bansi-Matharu L, Law M, Zangerle R, Rauch A, Tarr PE, Greenberg L, Neesgaard B, Jaschinski N, De Wit S, Wit F, d'Arminio Monforte A, Fontas E, Castagna A, Stecher M, Florence E, Begovac J, Mussini C, Sönnerborg A, Abutidze A, Groh A, Vannappagari V, Cohen C, Young L, Hosein S, Ryom L, Petoumenos K.   +26 more
europepmc   +3 more sources