Results 21 to 30 of about 16,702 (172)

HIV Integrase Inhibitors

, 2013
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 also outline areas for further improvement.
Mathieu Métifiot, Christophe Marchand, Yves Pommier   +2 more
openaire   +3 more sources

Screening of the NIH Clinical Collection for inhibitors of HIV-1 integrase activity

South African Journal of Science, 2018
Drug repurposing offers a validated approach to reduce drug attrition within the drug discovery and development pipeline through the application of known drugs and drug candidates to treat new indications.
Shaakira Abrahams, Salerwe Mosebi, Muhammed Q. Fish, Maria A. Papathanasopoulos, Raymond Hewer   +4 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

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

Discovery of Novel Integrase Inhibitors Acting outside the Active Site Through High-Throughput Screening

Molecules, 2019
Currently, an increasing number of drugs are becoming available to clinics for the treatment of HIV infection. Even if this targeted therapy is highly effective at suppressing viral replication, caregivers are facing growing therapeutic failures in ...
Cindy Aknin, Elena A. Smith, Christophe Marchand, Marie-Line Andreola, Yves Pommier, Mathieu Metifiot   +5 more
doaj   +1 more source

HIV-1 resistance patterns to integrase inhibitors in Chilean patients with virological failure on raltegravir-containing regimens

Journal of Virus Eradication, 2020
In this viewpoint we would like to describe our results in terms of resistance pattern in Chilean patients with virological failure (VF) on raltegravir (RAL)-containing-regimens and highlight the need for the concomitant availability of genotypic ...
Pablo Ferrer, Consuelo Rodriguez, Alicia Sciaraffia, Rocío Tordecilla, Veronica Ramos, Magdalena Durán, Carlos Beltrán, Alejandro Afani   +7 more
doaj   +1 more source

Lipid Nanoparticles for the Delivery of CRISPR/Cas9 Machinery to Enable Site‐Specific Integration of CFTR and Mutation‐Agnostic Disease Rescue

Advanced Functional Materials, EarlyView.
Lipid nanoparticles (LNPs) are optimized to co‐deliver Cas9‐encoding messenger RNA (mRNA), a single guide RNA (sgRNA) targeting the endogenous cystic fibrosis transmembrane conductance regulator (CFTR) gene, and homologous linear double‐stranded donor DNA (ldsDNA) templates encoding CFTR.
Ruth A. Foley, Paul G. Ayoub, Vrishti Sinha, Colin Juett, Alicia Sanoyca, Emily C. Duggan, Lindsay E. Lathrop, Priyanka Bhatt, Kevin Coote, Beate Illek, Brigitte N. Gomperts, Donald B. Kohn, Steven J. Jonas   +12 more
wiley   +1 more source

Rational Design of Optical Single‐Walled Carbon Nanotube‐Based Nanosensors with Biological Recognition Elements

Advanced Sensor Research, EarlyView.
This Review focuses on assessing and providing perspective on the field of rationally‐designed optical sensors constructed with single‐walled carbon nanotubes. The literature is reviewed and evaluated for SWCNT‐based sensors constructed with biomolecular recognition elements, including proteins, peptides, and oligonucleotides, as well as their methods ...
Amelia K. Ryan, Atara Israel, Maria Celina Stefoni, Catarina Ferraz, Ryan M. Williams   +4 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

Viral Dynamic Model of Antiretroviral Therapy Including the Integrase Inhibitor Raltegravir in Patients with HIV-1

Biomath, 2012
Antiviral combination therapies consisting of reverse transcriptase inhibitors, protease inhibitors and an integrase inhibitor, have been developed to suppress HIV below the limit of detection.
Dimitra Bon, Christoph Stephan, Oliver Keppler, Eva Herrmann   +3 more
doaj   +1 more source