Results 61 to 70 of about 28,079 (244)

Probing chelation motifs in HIV integrase inhibitors [PDF]

Proceedings of the National Academy of Sciences, 2012
A series of HIV integrase (HIV-1 IN) inhibitors were synthesized to evaluate the role of the metal-binding group (MBG) in this class of metalloenzyme inhibitors. A total of 21 different raltegravir-chelator derivative (RCD) compounds were prepared that differed only in the nature of the MBG.
Shahrzad Rostami, Jamie Desoto, Yves Pommier, Arpita Agrawal, Seth M. Cohen, Jessica L. Fullagar, Douglas D. Richman, Kasthuraiah Maddali   +7 more
openaire   +3 more sources

Approaches to repurposing reverse transcriptase antivirals in cancer

British Journal of Clinical Pharmacology, EarlyView.
This review highlights the role of reverse transcriptase (RT) inhibition in cellular regulation associated with non‐terminal repeat retrotransposons and endogenous retroviruses. Based on their pleiotropic characteristics, RT inhibitors (RTIs) are discussed as potential anticancer agents.
Richard Head, Saiful Islam, Jennifer H. Martin   +2 more
wiley   +1 more source

Histone H2AX Is Phosphorylated at Sites of Retroviral DNA Integration but Is Dispensable for Postintegration Repair [PDF]

, 2004
The histone variant H2AX is rapidly phosphorylated (denoted {gamma}H2AX) in large chromatin domains (foci) flanking double strand DNA (dsDNA) breaks that are produced by ionizing radiation or genotoxic agents and during V(D)J recombination.
Bonner, William, Daniel, René, Greger, James G., Katz, Richard A., Nussenzweig, Andre, Ramcharan, Joseph, Rogakou, Emmy, Skalka, Anna Marie, Taganov, Konstantin D.   +8 more
core   +1 more source

Factors Influencing the Binding of HIV‐1 Protease Inhibitors: Insights from Machine Learning Models

ChemMedChem, Accepted Article.
HIV‐1 protease inhibitors are crucial for antiviral therapies targeting acquired immunodeficiency syndrome (AIDS). Hundreds of HIV‐1 protease complexes with various ligands have been resolved and deposited in the Protein Data Bank. However, binding affinity measurements for these ligands are not always available.
Yaffa Shalit, Inbal Tuvi-Arad
wiley   +1 more source

HIV-1 acquired drug resistance to integrase inhibitors in a cohort of antiretroviral therapy multi-experienced Mexican patients failing to raltegravir: a cross-sectional study

AIDS Research and Therapy, 2020
Background In resource-limited settings, multi-experienced HIV infected patients are often prescribed raltegravir for salvage therapy. Patients failing raltegravir-containing regimens require other drugs including other integrase inhibitors.
Aurelio Orta-Resendiz, Roberto A. Rodriguez-Diaz, Luis A. Angulo-Medina, Mario Hernandez-Flores, Luis E. Soto-Ramirez   +4 more
doaj   +1 more source

Discovery of a novel 5-carbonyl-1H-imidazole-4-carboxamide class of inhibitors of the HIV-1 integrase–LEDGF/p75 interaction [PDF]

Though much progress has been made in the inhibition of HIV-1 integrase catalysis, clinical resistance mutations have limited the promise of long-term drug prescription. Consequently, allosteric inhibition of integrase activity has emerged as a promising
Christ, Frauke, Debnath, Bikash, Debyser, Zeger, Long, Ya-Qiu, Neamati, Nouri, Serrao, Erik, Xu, Zhong-Liang   +6 more
core   +1 more source

Incorporation of aptamers in the terminal loop of shRNAs yields an effective and novel combinatorial targeting strategy. [PDF]

, 2017
Gene therapy by engineering patient's own blood cells to confer HIV resistance can potentially lead to a functional cure for AIDS. Toward this goal, we have previously developed an anti-HIV lentivirus vector that deploys a combination of shRNA, ribozyme ...
Castanotto, Daniela, Li, Haitang, Pang, Ka Ming, Rossi, John J, Scherer, Lisa   +4 more
core   +1 more source

A Randomized Phase 1 Study Evaluating Pharmacokinetics, Safety, and Tolerability of a High‐Concentration, Long‐Acting Cabotegravir Formulation in Adults Without HIV

Clinical Pharmacology in Drug Development, EarlyView.
Abstract Long‐acting (LA) cabotegravir 200‐mg/mL (CAB200) injections are approved for HIV‐1 prevention and as a complete LA HIV‐1 treatment regimen with rilpivirine. A high‐concentration suspension formulation, cabotegravir 400 mg/mL (CAB400‐D), was developed to enable less frequent dosing and self‐administration. This phase 1, double‐blind, randomized
Kelong Han, Paul Benn, Jörg Sievers, David Dorey, Michael Warwick‐Sanders, Randa Hareedy, Louise Harkness, Claudia Leemereise, Kjersten Offenbecker, Christina Donatti, Darin B. Brimhall, Christian Schwabe, Craig Boyle, Michael A. Hassman, Steve Knowles, Ronald D'Amico, William R. Spreen   +16 more
wiley   +1 more source

Resistance to inhibitors of the human immunodeficiency virus type 1 integration

Brazilian Journal of Infectious Diseases, 2010
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 infection.
Daria J. Hazuda, PhD
doaj  

Nature Inspired Delivery Vehicles for CRISPR‐Based Genome Editing

Small, EarlyView.
The review highlights nature‐inspired nanocarriers for CRISPR delivery, emphasizing viral vectors, extracellular vesicles, liposomes, and lipid nanoparticles. It discusses their roles in improving specificity, minimizing immunogenicity, and overcoming barriers in genome editing. Recent advancements, challenges, and therapeutic applications are explored,
Elizabeth Maria Clarissa, Mamata Karmacharya, Hyunmin Choi, Sumit Kumar, Yoon‐Kyoung Cho   +4 more
wiley   +1 more source