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
Novel therapeutic strategies targeting HIV integrase
BMC Medicine, 2012 Integration of the viral genome into host cell chromatin is a pivotal and unique step in the replication cycle of retroviruses, including HIV. Inhibiting HIV replication by specifically blocking the viral integrase enzyme that mediates this step is an ...
Quashie Peter K +2 more
doaj +1 more source
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
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
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 [PDF]
, 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 +4 more
core +2 more sources
Resistance to novel drug classes [PDF]
, 2009 Understanding the mechanisms that underlie resistance development to novel drugs is essential to a better clinical management of resistant viruses and to prevent further resistance development and spread. RECENT FINDINGS: Integrase inhibitors and CCR5
Calvez, V. +3 more
core +1 more source
mBio, 2017 Resistance to the integrase strand transfer inhibitors raltegravir and elvitegravir is often due to well-identified mutations in the integrase gene. However, the situation is less clear for patients who fail dolutegravir treatment.
Isabelle Malet +7 more
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