Results 31 to 40 of about 22,886 (216)

Histone deacetylase 1 interacts with HIV-1 Integrase and modulates viral replication

Virology Journal, 2019
Background HIV-1 hijacks the cellular machinery for its own replication through protein-protein interactions between viral and host cell factors. One strategy against HIV-1 infection is thus to target these key protein complexes.
Fadila Larguet, Clément Caté, Benoit Barbeau, Eric Rassart, Elsy Edouard   +4 more
doaj   +1 more source

GCN2 phosphorylates HIV-1 integrase and decreases HIV-1 replication by limiting viral integration

Scientific Reports, 2017
GCN2 is a serine/threonine kinase involved in cellular stress response related to amino acid starvation. Previously, we showed that GCN2 interacts with HIV-1 integrase and is activated during HIV-1 infection.
A. Jaspart, C. Calmels, O. Cosnefroy, P. Bellecave, P. Pinson, S. Claverol, V. Guyonnet-Dupérat, B. Dartigues, M. S. Benleulmi, E. Mauro, P. A. Gretteau, V. Parissi, M. Métifiot, M. L. Andreola   +13 more
doaj   +1 more source

HIV-1 Subtype C Drug Resistance Mutations in Heavily Treated Patients Failing Integrase Strand Transfer Inhibitor-Based Regimens in Botswana

Viruses, 2021
There are limited real-world mutational and virological outcomes data of treatment-experienced persons diagnosed with HIV-1 subtype C (HIV-1 C) who are failing Integrase Strand Transfer Inhibitor-based regimens. Requisition forms sent for HIV-1 genotypic
Kaelo K. Seatla, Dorcas Maruapula, Wonderful T. Choga, Tshenolo Ntsipe, Nametso Mathiba, Mompati Mogwele, Max Kapanda, Bornapate Nkomo, Dinah Ramaabya, Joseph Makhema, Mompati Mmalane, Madisa Mine, Ishmael Kasvosve, Shahin Lockman, Sikhulile Moyo, Simani Gaseitsiwe   +15 more
doaj   +1 more source

Integrase Inhibitor Prodrugs: Approaches to Enhancing the Anti-HIV Activity of β-Diketo Acids

Molecules, 2015
HIV integrase, encoded at the 3′-end of the HIV pol gene, is essential for HIV replication. This enzyme catalyzes the incorporation of HIV DNA into human DNA, which represents the point of “no-return” in HIV infection.
Vasu Nair, Maurice Okello
doaj   +1 more source

Emergence of the G118R Pan-Integrase Resistance Mutation as a Result of Low Compliance to a Dolutegravir-Based cART

Infectious Disease Reports, 2022
HIV-1 resistance towards integrase inhibitors is a potential threat of the success of HIV-1 combination treatment. G118R is a rare drug resistance mutation conferring pan-integrase resistance.
Helene Mens, Lasse Fjordside, Jannik Fonager, Jan Gerstoft   +3 more
doaj   +1 more source

CoMFA and CoMSIA Studies on Inhibitors of HIV-1 Integrase - Bicyclic Pyrimidinones

E-Journal of Chemistry, 2010
To understand the structural requirements of HIV-1 integrase inhibitors and to design new ligands against human HIV-1 integrase with enhanced inhibitory potency, a 3D QSAR (quantitative structure-activity relationship) study with comparative molecular ...
V. Radhika, S. Sree Kanth, M. Vijjulatha
doaj   +1 more source

HIV-1 integrase polymorphisms are associated with prior antiretroviral drug exposure

Retrovirology, 2009
In a recent summary of integrase sequences, primary integrase inhibitor mutations were rare. In a review of integrase inhibitor-naïve Australian HIV-1 sequences, primary mutations were not identified, although the accessory mutation G140S was detected. A
Wang Bin, Deris Zaquan, Herring Belinda, van Hal Sebastiaan J, Saksena Nitin K, Dwyer Dominic E   +5 more
doaj   +1 more source

Delivery of Islatravir via High Drug‐Load, Long‐acting Microarray Patches for the Prevention or Treatment of Human Immunodeficiency Virus

Advanced Healthcare Materials, Volume 14, Issue 7, March 14, 2025.
Islatravir‐loaded dissolving microarray patches (MAPs) provide a minimally invasive, long‐acting solution for HIV‐1 prevention and treatment. In rats, sustained islatravir delivery lasts up to three months, while in minipigs, efficacious plasma levels are detected for six days.
Qonita Kurnia Anjani, Ashley R. Johnson, Akmal H. Sabri, Ryan Lutz, Steven Tignor, Jeanine Ballard, Nathan Rudd, Li Zhao, Lalitkumar K. Vora, Stephanie E. Barrett, Angela Wagner, Ryan F. Donnelly   +11 more
wiley   +1 more source

Resistance to inhibitors of the human immunodeficiency virus type 1 integration

Brazilian Journal of Infectious Diseases
This review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 ...
Daria J Hazuda
doaj   +1 more source

Direct Access to α,β‐Unsaturated γ‐Lactams via Palladium‐Catalysed Carbonylation of Propargylic Ureas.

Advanced Synthesis &Catalysis, Volume 367, Issue 5, March 4, 2025.
Abstract Additive carbonylations typically necessitate strong nucleophiles, such as alcohols or amines. In this study, we carbonylated a poorly nucleophilic urea, under oxidant‐free conditions. Our straightforward carbonylative strategy enables access to versatile α,β‐unsaturated γ‐lactams featuring an aminocarbonyl fragment, utilizing readily ...
Debora Schiroli, Aleksandr Voronov, Francesco Pancrazzi, Nunzio Iraci, Salvatore Vincenzo Giofrè, Beatrice Macchi, Valeria Stefanizzi, Raffaella Mancuso, Bartolo Gabriele, Paolo Pio Mazzeo, Luca Capaldo, Nicola Della Ca'   +11 more
wiley   +1 more source