Results 21 to 30 of about 17,346 (194)

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

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

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

Reciprocal control of viral infection and phosphoinositide dynamics

FEBS Letters, EarlyView.
Phosphoinositides, although scarce, regulate key cellular processes, including membrane dynamics and signaling. Viruses exploit these lipids to support their entry, replication, assembly, and egress. The central role of phosphoinositides in infection highlights phosphoinositide metabolism as a promising antiviral target.
Marie Déborah Bancilhon, Bruno Mesmin
wiley   +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

Importin 7 mediates the nuclear import of HIV‐1 integrase via a specific interacting interface

FEBS Open Bio, EarlyView.
HIV‐1 integrase enables viral DNA integration into the host genome. By binding to the core domain of the host protein Importin 7 via its C‐terminal domain, the integrase is transported across the nuclear membrane into the nucleus, where integration of the viral genome into host DNA takes place. This translocation is a critical step for subsequent viral
Juana Bana, Avigail Yariv, Tal Oppenheim, Hadar Amartely, Dana Reichmann, Oded Livnah   +5 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

Discovery and Engineering of a Rat Endogenous Retrovirus Reverse Transcriptase for Efficient Prime Editing

Advanced Science, EarlyView.
We screened 558 reverse transcriptases and engineered an optimized rat endogenous retrovirus‐derived variant, enRERV‐RT, via structure‐guided engineering and deep mutational scanning. This enhanced prime editor, based on the engineered RT, outperforms conventional M‐MLV‐RT systems across plant and animal cells, particularly at hard‐to‐edit loci ...
Linsha Ma, Pengcheng Yao, Shengqi Wu, Yuanyuan Shi, Lang Qin, Baitao Li, Jiayi Zhu, Minhua Huang, Yichong Zhu, Yuwen Song, Jinhuan Pang, Ziping Guo, Guochuan Wu, Chen Wang, Kewei Xu, Ruihua Huang, Quan Kuang, Liang Qu, Changtian Pan, Xianrong Xie, Qinlong Zhu, Jiaying Huang, Qiupeng Lin   +22 more
wiley   +1 more source

Multi-Substituted Quinolines as HIV-1 Integrase Allosteric Inhibitors

Viruses, 2022
Allosteric HIV-1 integrase (IN) inhibitors, or ALLINIs, are a new class of antiviral agents that bind at the dimer interface of the IN, away from the enzymatic catalytic site and block viral replication by triggering an aberrant multimerization of the ...
Long Phi Dinh, Jian Sun, Courtney D. Glenn, Krunal Patel, Julie A. Pigza, Matthew G. Donahue, Larry Yet, Jacques J. Kessl   +7 more
doaj   +1 more source