Incorporation of aptamers in the terminal loop of shRNAs yields an effective and novel combinatorial targeting strategy. [PDF]
Gene therapy by engineering patient's own blood cells to confer HIV resistance can potentially lead to a functional cure for AIDS. Toward this goal, we have previously developed an anti-HIV lentivirus vector that deploys a combination of shRNA, ribozyme ...
Castanotto, Daniela +4 more
core +1 more source
Drug resistance in B and non-B subtypes amongst subjects recently diagnosed as primary/recent or chronic HIV-infected over the period 2013–2016: Impact on susceptibility to first-line strategies including integrase strand-transfer inhibitors [PDF]
Objectives To characterize the prevalence of transmitted drug resistance mutations (TDRMs) by plasma analysis of 750 patients at the time of HIV diagnosis from January 1, 2013 to November 16, 2016 in the Veneto region (Italy), where all drugs included in
Alvarez, M +18 more
core +1 more source
Effectiveness of dolutegravir-based regimens as either first-line or switch antiretroviral therapy: data from the Icona cohort [PDF]
Introduction: Concerns about dolutegravir (DTG) tolerability in the real-life setting have recently arisen. We aimed to estimate the risk of treatment discontinuation and virological failure of DTG-based regimens from a large cohort of HIV-infected ...
Abeli C. +155 more
core +4 more sources
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
Resistance against Integrase Strand Transfer Inhibitors and Relevance to HIV Persistence
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
The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function
Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are an emerging class of small molecules that disrupt viral maturation by inducing the aberrant multimerization of IN. Here, we present cocrystal structures of HIV-1 IN with two potent ALLINIs, namely,
Matthew R. Singer +14 more
doaj +1 more source
Modeling the HIV-1 Intasome: A Prototype View of the Target of Integrase Inhibitors
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]
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
Targeting STAT3 in Cancer with Nucleotide Therapeutics. [PDF]
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 +3 more
core +2 more sources
Nonhuman Primates and Humanized Mice for Studies of HIV-1 Integrase Inhibitors: A Review
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 +2 more
doaj +1 more source

