Results 21 to 30 of about 2,882,240 (203)

Pharmacokinetic drug interactions of integrase strand transfer inhibitors

Current Research in Pharmacology and Drug Discovery, 2021
The integrase strand transfer inhibitor (INSTI)-containing regimens are currently considered as the first-line treatment of human immunodeficiency virus (HIV) infection. Although possessing a common mechanism of action to inhibit HIV integrase irreversibly to stop HIV replication cycle, the INSTIs, including raltegravir, elvitegravir, dolutegravir, and
Chi-Hua Lu, Edward M. Bednarczyk, Linda M. Catanzaro, Alyssa Shon, Jia-Chen Xu, Qing Ma   +5 more
openaire   +3 more sources

HIV-1 Integrase Strand Transfer Inhibitors and Neurodevelopment

Pharmaceuticals, 2022
Children born to mothers, with or at risk, of human immunodeficiency virus type-1 (HIV-1) infection are on the rise due to affordable access of antiretroviral therapy (ART) to pregnant women or those of childbearing age. Each year, up to 1.3 million HIV-1-infected women on ART have given birth with recorded mother-to-child HIV-1 transmission rates of ...
Emma G. Foster, Howard E. Gendelman, Aditya N. Bade   +2 more
openaire   +3 more sources

Integrase Strand Transfer Inhibitors in HIV Therapy [PDF]

Infectious Diseases and Therapy, 2013
HIV drug resistance has been one of the major obstacles to HIV eradication and has contributed to the need for the constant development of new antiretroviral drugs over the past 25 years. With the recent approval of dolutegravir for human therapy by the U.S.
Mesplède, Thibault, Wainberg, Mark A.
openaire   +2 more sources

Cryo-EM structure of the Rous sarcoma virus octameric cleaved synaptic complex intasome

Communications Biology, 2021
Pandey, Bera, Shi et al. report the cryo-electron microscopy structure of the Rous sarcoma virus octameric intasome complex stabilized by a HIV-1 integrase strand transfer inhibitor.
Krishan K. Pandey, Sibes Bera, Ke Shi, Michael J. Rau, Amarachi V. Oleru, James A. J. Fitzpatrick, Alan N. Engelman, Hideki Aihara, Duane P. Grandgenett   +8 more
doaj   +1 more source

Structural basis for the inhibition of HTLV-1 integration inferred from cryo-EM deltaretroviral intasome structures

Nature Communications, 2021
Human T-cell lymphotropic virus type 1 (HTLV-1) is an oncogenic deltaretrovirus. Here the authors provide structural characterization of the binding mechanism of novel integrase strand transfer inhibitor (INSTI) candidates to limit HTLV-1 infection.
Michal S. Barski, Teresa Vanzo, Xue Zhi Zhao, Steven J. Smith, Allison Ballandras-Colas, Nora B. Cronin, Valerie E. Pye, Stephen H. Hughes, Terrence R. Burke, Peter Cherepanov, Goedele N. Maertens   +10 more
doaj   +1 more source

Differential Sensitivities of Retroviruses to Integrase Strand Transfer Inhibitors [PDF]

Journal of Virology, 2011
ABSTRACT Integrase inhibitors are emerging anti-human immunodeficiency virus (HIV) drugs, and multiple retroviruses and transposable elements were evaluated here for susceptibilities to raltegravir (RAL) and elvitegravir (EVG).
Koh, Yasuhiro, Matreyek, Kenneth A., Engelman, Alan   +2 more
openaire   +4 more sources

Primary resistance against integrase strand transfer inhibitors in integrase strand transfer inhibitor-naive patients failing first- and second-line ART in Tanzania. [PDF]

J Antimicrob Chemother, 2022
Abstract Introduction Sub-Saharan African countries are introducing integrase strand transfer inhibitors (INSTIs) in their ART programmes as the preferred first-line regimen, and dolutegravir is the INSTI of choice due to its potency, tolerability and high genetic barrier to resistance.
Henerico S, Lyimo E, Makubi AN, Magesa D, Desderius B, Mueller A, Changalucha J, Kalluvya SE, Van Zyl G, Preiser W, Mshana SE, Kasang C.   +11 more
europepmc   +3 more sources

Structural Biology of HIV Integrase Strand Transfer Inhibitors

Trends in Pharmacological Sciences, 2020
Integrase (IN) strand transfer inhibitors (INSTIs) are recent compounds in the antiretroviral arsenal used against HIV. INSTIs work by blocking retroviral integration; an essential step in the viral lifecycle that is catalyzed by the virally encoded IN protein within a nucleoprotein assembly called an intasome. Recent structures of lentiviral intasomes
Ilona K. Jóźwik, Dario O. Passos, Dmitry Lyumkis   +2 more
openaire   +3 more sources

Different Pathways Conferring Integrase Strand-Transfer Inhibitors Resistance

Viruses, 2022
Integrase Strand Transfer Inhibitors (INSTIs) are currently used as the most effective therapy in the treatment of human immunodeficiency virus (HIV) infections. Raltegravir (RAL) and Elvitegravir (EVG), the first generation of INSTIs used successfully in clinical treatment, are susceptible to the emergence of viral resistance and have a high rate of ...
Richetta, Clémence, Quang Tu, Nhat, Delelis, Olivier   +2 more
openaire   +3 more sources

Structural Studies of the HIV-1 Integrase Protein: Compound Screening and Characterization of a DNA-Binding Inhibitor. [PDF]

PLoS ONE, 2015
Understanding the HIV integrase protein and mechanisms of resistance to HIV integrase inhibitors is complicated by the lack of a full length HIV integrase crystal structure. Moreover, a lentiviral integrase structure with co-crystallised DNA has not been
Peter K Quashie, Ying-Shan Han, Said Hassounah, Thibault Mesplède, Mark A Wainberg   +4 more
doaj   +1 more source