Results 41 to 50 of about 633,523 (228)

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

Dual‐line Genome‐scale CRISPR Screening Enables Robust Target Gene Discovery

Advanced Science, EarlyView.
A species‐optimized CRISPR platform integrates efficient piggyBac delivery, genome‐scale sgRNA libraries, and parallel screening in two independently engineered Bactrocera dorsalis Cas9 cell lines. Cross‐line consensus analysis filters line‐specific effects, enriches candidates with reproducible in vivo phenotypes, and reveals conserved, species ...
Ziniu Li, Jiao Qiao, Qiuyuan Zhang, Peipei Liu, Chenjun Zheng, Qi Zhou, Mengqi Ji, Zhihui Zhu, Xiaoxue Li, Hongyu Zhang   +9 more
wiley   +1 more source

In Vivo Direct Reprogramming: Current Progress and Future Prospects from Mechanisms to Therapeutic Application

Advanced Science, EarlyView.
This review examines the potential of in vivo direct reprogramming in regenerative medicine for functional tissue restoration, highlighting the role of tissue‐resident cues in generating functionally mature reprogrammed cells from lineage‐related cells. It contains a discussion on mechanisms, reprogramming factors, delivery approaches, and applications
Rishabh Deo Singh, Mauro Calvoli, Kyeong Kyu Kim   +2 more
wiley   +1 more source

Determination of Gene‐Level Fitness Contributions Across the Mucin‐Utilization Network of Bacteroides thetaiotaomicron

Advanced Science, EarlyView.
Genome‐wide CRISPRi and RNA‐seq resolve how B. thetaiotaomicron converts host mucosal glycans into fitness. The study reveals a layered mucin‐utilization architecture in which capsular polysaccharides constrain surface access, extracellular CAZymes and peptidases show functional redundancy, and intracellular catabolic pathways create discrete metabolic
Kangsan Kim, Jiwon Lee, Minjeong Kang, Sung Sun Yim, Donghui Choe, Byung‐Kwan Cho   +5 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

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

Structure of a HIV-1 IN-Allosteric inhibitor complex at 2.93 Å resolution: Routes to inhibitor optimization.

PLoS Pathogens, 2023
HIV integrase (IN) inserts viral DNA into the host genome and is the target of the strand transfer inhibitors (STIs), a class of small molecules currently in clinical use.
Grant Eilers, Kushol Gupta, Audrey Allen, Saira Montermoso, Hemma Murali, Robert Sharp, Young Hwang, Frederic D Bushman, Gregory Van Duyne   +8 more
doaj   +1 more source

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.
Emma G. Foster, Howard E. Gendelman, Aditya N. Bade   +2 more
doaj   +1 more source

Pharmacogenomics of dolutegravir: A scoping review of evidence, gaps and clinical implications

British Journal of Clinical Pharmacology, EarlyView.
Dolutegravir underpins modern first‐ and second‐line HIV treatment regimens; however, interindividual variability in its disposition and tolerability presents challenges for optimal use. This scoping review mapped current evidence on the pharmacogenomics of dolutegravir, focusing on pharmacokinetics and pharmacodynamics, and methodological limitations ...
Ronald Kiguba, Mishael Ssesanga, Munir Pirmohamed   +2 more
wiley   +1 more source

A Fluorescent Assay to Search for Inhibitors of HIV-1 Integrase Interactions with Human Ku70 Protein, and Its Application for Characterization of Oligonucleotide Inhibitors

Biomolecules, 2020
The search for compounds that can inhibit the interaction of certain viral proteins with their cellular partners is a promising trend in the development of antiviral drugs.
Simon Galkin, Anna Rozina, Arthur Zalevsky, Marina Gottikh, Andrey Anisenko   +4 more
doaj   +1 more source