Results 41 to 50 of about 3,561 (181)

Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV‑1 Integrase Inhibitors

, 2020
The standard of care for HIV-1 infection, highly active antiretroviral therapy (HAART), combines two or more drugs from at least two classes. Even with the success of HAART, new drugs with novel mechanisms are needed to combat viral resistance, improve ...
Guo Li (174860), Ira B. Dicker (2618830), Christopher Cianci (6240926), Susan Jenkins (1834318), Javed A. Khan (1551379), Mark R. Krystal (5141438), Zeyu Lin (2618836), Hal Lewis (1442743), George L. Trainor (1436416), Tricia Protack (2618848), Prasanna Sivaprakasam (1399360), Linda Discotto (8474724), Samuel W. Gerritz (312377), Alicia Ng (1442749), Nicholas A. Meanwell (362044), David R. Langley (367086), Michael A. Walker (1754566), Kevin Kish (1399378), Annapurna Pendri (362039), B. Narasimhulu Naidu (2686801)   +19 more
core   +2 more sources

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

Streptavidins Coordinate Biotin Sequestration and Self‐Resistance Within a Biotin‐Pathway Antibiotic Network

Advanced Science, EarlyView.
A conserved genomic region between two streptavidin genes in Streptomyces packages biosynthetic gene clusters for diverse biotin‐pathway antibiotics: acidomycin, stravidin, the new non‐proteinogenic amino acid ANDA, and the new BioA inhibitor α‐methyl‐KAPA.
Sumire Kurosawa, Jingjun Mo, Xiaotong Diao, Feng Xie, Tingting Wang, Haowen Zhao, Dalei Wu, Rolf Müller, Chengzhang Fu   +8 more
wiley   +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

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

HIV Dynamics and Integrase Inhibitors

Antiviral Chemistry and Chemotherapy, 2009
The integrase inhibitor (INI) raltegravir has shown promising results in clinical trials to date, reducing second phase HIV RNA levels by 70% in comparison with standard regimens. These trial results have been limited by the 50 copies/ml detection limit of the HIV RNA assay and have not investigated the effect of an INI regimen on levels of latently ...
openaire   +2 more sources

RNA‐centric world of retroviruses: unravelling the molecular strategies of genomic RNA packaging

Biological Reviews, EarlyView.
ABSTRACT Retroviruses constitute a unique group of RNA viruses that have profoundly influenced both evolutionary trajectories and biomedical research. Their ability to reverse transcribe and integrate into host genomes has shaped genomic architecture across species and contributed to our understanding of oncogenes, gene regulation, and RNA biology ...
Mohammad Abdullah Jehad, Suresha G. Prabhu, Lizna M. Ali, Vineeta N. Pillai, Farah Mustafa, Tahir A. Rizvi   +5 more
wiley   +1 more source

Computer tools in the discovery of HIV-1 integrase inhibitors

, 2010
Computer-aided drug design (CADD) methodologies have made great advances and contributed significantly to the discovery and/or optimization of many clinically used drugs in recent years.
Chenzhong Liao, Marc C Nicklaus
core   +1 more source

Characterization of HIV-1 Integrase Gene and Resistance Associated Mutations Prior to Roll out of Integrase Inhibitors by Kenyan National HIV-Treatment Program in Kenya

, 2020
BACKGROUND: Antiretroviral therapy containing an integrase strand transfer inhibitor plus two Nucleoside Reverse Transcriptase inhibitors has now been recommended for treatment of HIV-1-infected patients.
Lihana Raphael, Sepha, Mabeya, Nyerere Andrew, Nyamache Anthony, Ngugi Caroline   +4 more
core   +1 more source