Results 91 to 100 of about 2,808,349 (298)

Approaches to repurposing reverse transcriptase antivirals in cancer

British Journal of Clinical Pharmacology, EarlyView.
This review highlights the role of reverse transcriptase (RT) inhibition in cellular regulation associated with non‐terminal repeat retrotransposons and endogenous retroviruses. Based on their pleiotropic characteristics, RT inhibitors (RTIs) are discussed as potential anticancer agents.
Richard Head, Saiful Islam, Jennifer H. Martin   +2 more
wiley   +1 more source

HIV integrase inhibitor, Elvitegravir, impairs RAG functions and inhibits V(D)J recombination

Cell Death and Disease, 2017
Integrase inhibitors are a class of antiretroviral drugs used for the treatment of AIDS that target HIV integrase, an enzyme responsible for integration of viral cDNA into host genome.
Mayilaadumveettil Nishana, N. Nilavar, Rupa Kumari, Monica Pandey, S. Raghavan   +4 more
semanticscholar   +1 more source

Pyrone-based inhibitors of metalloproteinase types 2 and 3 may work as conformation-selective inhibitors. [PDF]

, 2011
Matrix metalloproteinases are zinc-containing enzymes capable of degrading all components of the extracellular matrix. Owing to their role in human disease, matrix metalloproteinase have been the subject of extensive study.
de Oliveira, César AF, Durrant, Jacob D, McCammon, J Andrew   +2 more
core   +1 more source

Factors Influencing the Binding of HIV‐1 Protease Inhibitors: Insights from Machine Learning Models

ChemMedChem, EarlyView.
Machine learning unlocks the secrets of HIV‐1 protease inhibition, paving the way for data‐driven antiviral drug design. This study analyzes crystallographic data from hundreds of protein–ligand complexes, predicting ligand binding affinity with over 85% accuracy.
Yaffa Shalit, Inbal Tuvi‐Arad
wiley   +1 more source

Resistance to inhibitors of the human immunodeficiency virus type 1 integration

Brazilian Journal of Infectious Diseases, 2010
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 infection.
Daria J. Hazuda, PhD
doaj  

Dolutegravir-Associated Hyperglycemia in a Patient on Highly Active Antiretroviral Therapies

Nigerian Journal of Medicine
Highly active antiretroviral medications have been reported to cause hyperglycaemia in the literature especially the protease inhibitor. We however report a case of dolutegravir-associated hyperglycaemia which is an integrase strand transfer inhibitor.
Abosede Grace Adeyeye, Victor Oladeji Adeyeye   +1 more
doaj   +1 more source

The Competitive Interplay between Allosteric HIV-1 Integrase Inhibitor BI/D and LEDGF/p75 during the Early Stage of HIV-1 Replication Adversely Affects Inhibitor Potency.

ACS Chemical Biology, 2016
Allosteric HIV-1 integrase inhibitors (ALLINIs) have recently emerged as a promising class of antiretroviral agents and are currently in clinical trials. In infected cells, ALLINIs potently inhibit viral replication by impairing virus particle maturation
Lei Feng, V. Dharmarajan, Erik Serrao, Ashley C Hoyte, Ross C. Larue, Alison Slaughter, Amit Sharma, Matthew R. Plumb, J. Kessl, J. Fuchs, F. Bushman, A. Engelman, P. Griffin, M. Kvaratskhelia   +13 more
semanticscholar   +1 more source

Targeting STAT3 in Cancer with Nucleotide Therapeutics. [PDF]

, 2019
Signal transducer and activator of transcription 3 (STAT3) plays a critical role in promoting the proliferation and survival of tumor cells. As a ubiquitously-expressed transcription factor, STAT3 has commonly been considered an "undruggable" target for ...
Grandis, Jennifer R, Johnson, Daniel E, Lau, Yue-Ting K, Ramaiyer, Malini   +3 more
core   +2 more sources

Clinical Evaluation of Drug–Drug Interactions Between Bictegravir and Strong Inhibitors/Inducers of the CYP3A4, UGT1A1, or P‐gp Pathways

The Journal of Clinical Pharmacology, EarlyView.
Abstract In addition to antiretroviral therapy (ART), people with HIV often take medications to treat comorbidities. It is therefore important to assess these medications for potential drug‐drug interactions, which may affect the safety and efficacy of ART. Three phase I studies were conducted in adult participants without HIV. The pharmacokinetics (PK)
Priyanka Arora, Hui Liu, John Ling, Jason T. Hindman, Dhananjay D. Marathe   +4 more
wiley   +1 more source

Brief Histories of Retroviral Integration Research and Associated International Conferences

Viruses
The field of retroviral integration research has a long history that started with the provirus hypothesis and subsequent discoveries of the retroviral reverse transcriptase and integrase enzymes.
Duane P. Grandgenett, Alan N. Engelman
doaj   +1 more source