Microorganisms, 2021 Background: HIV infects around one hundred thousand patients in the Republic of the Congo. Approximately 25% of them receive an antiretroviral treatment; current first-line regimens include two NRTIs and one NNRTI, reverse transcriptase inhibitors ...
Ferdinand Emaniel Brel Got +7 more
doaj +1 more source
Allosteric HIV-1 integrase inhibitors lead to premature degradation of the viral RNA genome and integrase in target cells [PDF]
, 2017 Recent evidence indicates that inhibition of HIV-1 integrase (IN) binding to the viral RNA genome by allosteric integrase inhibitors (ALLINIs) or through mutations within IN yields aberrant particles in which the viral ribonucleoprotein complexes (vRNPs)
Elliott, Jennifer +8 more
core +2 more sources
Elvitegravir: A New HIV Integrase Inhibitor [PDF]
Antiviral Chemistry and Chemotherapy, 2009 Integration is a distinctive and essential process in the HIV infection cycle and thus represents an attractive antiviral drug target. Integrase inhibitors combined with other classes of drug might contribute to long-lasting suppression of HIV type-1 (HIV-1) replication for many patients.
Kazuya Shimura +2 more
openaire +3 more sources
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
Resistance against Integrase Strand Transfer Inhibitors and Relevance to HIV Persistence
Viruses, 2015 Drug resistance prevents the successful treatment of HIV-positive individuals by decreasing viral sensitivity to a drug or a class of drugs. In addition to transmitted resistant viruses, treatment-naïve individuals can be confronted with the problem of ...
Thibault Mesplède, Mark A. Wainberg
doaj +1 more source
New antiretroviral drugs [PDF]
, 2003 Despite the availability of 16 antiretroviral drugs approved for the treatment of HIV infection, current combination regimens present challenges. Newer antiretroviral drugs are needed to improve convenience, reduce toxicity and, of particular importance,
Gulick, R.M.
core +1 more source
Modeling the HIV-1 Intasome: A Prototype View of the Target of Integrase Inhibitors
Viruses, 2010 The HIV-1 integrase enzyme is essential for integrating the viral DNA into the host chromosome. Infection is aborted in the absence of integration, making integrase an attractive antiviral target. Recently approved inhibitors of integrase bind tightly to
Robert Craigie, Zhiqi Yin
doaj +1 more source
Molecular features related to HIV integrase inhibition obtained from structure- and ligand-based approaches. [PDF]
PLoS ONE, 2014 Among several biological targets to treat AIDS, HIV integrase is a promising enzyme that can be employed to develop new anti-HIV agents. The aim of this work is to propose a mechanistic interpretation of HIV-1 integrase inhibition and to rationalize the ...
Luciana L de Carvalho +5 more
doaj +1 more source
Integrase Strand Transfer Inhibitors in HIV Therapy [PDF]
Infectious Diseases and Therapy, 2013 HIV drug resistance has been one of the major obstacles to HIV eradication and has contributed to the need for the constant development of new antiretroviral drugs over the past 25 years. With the recent approval of dolutegravir for human therapy by the U.S.
Mark A. Wainberg +2 more
openaire +2 more sources
Dolutegravir-based regimen maintains virological success in a patient with archived mutations to integrase inhibitors [PDF]
, 2017 no abstract ...
Falasca, Francesca +3 more
core +1 more source