Results 21 to 30 of about 14,793 (172)

Nonhuman Primates and Humanized Mice for Studies of HIV-1 Integrase Inhibitors: A Review

Pathogens and Immunity, 2016
Since the discovery of the first inhibitors of HIV replication, drug resistance has been a major problem in HIV therapy, due, in part, to the high mutation rate of HIV.
Said A. Hassounah, Thibault Mesplède, Mark A. Wainberg   +2 more
doaj   +1 more source

Integrase Inhibitor Prodrugs: Approaches to Enhancing the Anti-HIV Activity of β-Diketo Acids

Molecules, 2015
HIV integrase, encoded at the 3′-end of the HIV pol gene, is essential for HIV replication. This enzyme catalyzes the incorporation of HIV DNA into human DNA, which represents the point of “no-return” in HIV infection.
Vasu Nair, Maurice Okello
doaj   +1 more source

HIV-1 integrase polymorphisms are associated with prior antiretroviral drug exposure

Retrovirology, 2009
In a recent summary of integrase sequences, primary integrase inhibitor mutations were rare. In a review of integrase inhibitor-naïve Australian HIV-1 sequences, primary mutations were not identified, although the accessory mutation G140S was detected. A
Wang Bin, Deris Zaquan, Herring Belinda, van Hal Sebastiaan J, Saksena Nitin K, Dwyer Dominic E   +5 more
doaj   +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

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

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

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

Molecular Epidemiology of HIV-1 in Eastern Europe and Russia

Viruses, 2022
The HIV epidemic in Eastern Europe and Russia is large and not well-controlled. To describe the more recent molecular epidemiology of HIV-1, transmitted drug resistance, and the relationship between the epidemics in this region, we sequenced the protease
Maarten A. A. van de Klundert, Anastasiia Antonova, Giulia Di Teodoro, Rafael Ceña Diez, Nikoloz Chkhartishvili, Eva Heger, Anna Kuznetsova, Aleksey Lebedev, Aswathy Narayanan, Ekaterina Ozhmegova, Alexander Pronin, Andrey Shemshura, Alexandr Tumanov, Nico Pfeifer, Rolf Kaiser, Francesco Saladini, Maurizio Zazzi, Francesca Incardona, Marina Bobkova, Anders Sönnerborg   +19 more
doaj   +1 more source

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

Visible‐Light‐Mediated Synthesis of Biscoumarins Utilizing Photocaged Sulfonic Acid as the Catalyst

European Journal of Organic Chemistry, EarlyView.
A mild visible light approach for the synthesis of biscoumarins utilizing arylazo sulfones as the photoacid generator under 467 nm irradiation is introduced. Throughout the years, biscoumarin derivatives, known for their diverse biological properties, have attracted extensive synthetic interest.
Athina S. J. Shkembi, Stamatis K. Serviou, Valentina Benazzi, Maurizio Fagnoni, Stefano Protti, Christoforos G. Kokotos   +5 more
wiley   +1 more source