Integrase and integration: biochemical activities of HIV-1 integrase [PDF]
Integration of retroviral DNA is an obligatory step of retrovirus replication because proviral DNA is the template for productive infection. Integrase, a retroviral enzyme, catalyses integration.
Deprez Eric +4 more
doaj +3 more sources
HIV-1 Integrase-DNA Recognition Mechanisms [PDF]
Integration of a reverse transcribed DNA copy of the HIV viral genome into the host chromosome is essential for virus replication. This process is catalyzed by the virally encoded protein integrase. The catalytic activities, which involve DNA cutting and
Mamuka Kvaratskhelia +5 more
doaj +3 more sources
Arylamide Inhibitors of HIV-1 Integrase
Based on data derived from a large number of HIV-1 integrase inhibitors, similar structural features can be observed, which consist of two aryl units separated by a central linker. For many inhibitors fitting this pattern, at least one aryl ring also requires ortho bis-hydroxylation for significant inhibitory potency.
He Zhao +5 more
openalex +3 more sources
HIV-1 Integrase T218I/S Polymorphisms Do Not Reduce HIV-1 Integrase Inhibitors' Phenotypic Susceptibility. [PDF]
The recently Food and Drug Administration (FDA)-approved cabotegravir (CAB) has demonstrated efficacy as an antiretroviral agent for HIV treatment and prevention, becoming an important tool to stop the epidemic in the United States of America (USA).
Rodríguez-López ER +9 more
europepmc +3 more sources
Authentic HIV-1 Integrase Inhibitors [PDF]
HIV-1 integrase (IN) is indispensable for HIV-1 replication and has become a validated target for developing anti-AIDS agents. In two decades of development of IN inhibition-based anti-HIV therapeutics, a significant number of compounds were identified as IN inhibitors, but only some of them showed antiviral activity.
Chenzhong, Liao +4 more
openaire +2 more sources
Fungal Phenalenones Inhibit HIV-1 Integrase [PDF]
A phenalenone compound, atrovenetinone methyl acetal, was isolated from a culture broth of Penicillium sp. FKI-1463 as an HIV-1 integrase inhibitor, and it showed anti-HIV activity in vitro. HIV-1 integrase inhibition and anti-HIV activity of two other natural phenalenones were also studied.
Kazuro, Shiomi +13 more
openaire +2 more sources
Integrase deficient lentiviral vector: prospects for safe clinical applications [PDF]
HIV-1 derived lentiviral vector is an efficient transporter for delivering desired genetic materials into the targeted cells among many viral vectors. Genetic material transduced by lentiviral vector is integrated into the cell genome to introduce new ...
Chee-Hong Takahiro Yew +6 more
doaj +2 more sources
Small molecule inhibitors of the LEDGF site of human immunodeficiency virus integrase identified by fragment screening and structure based design. [PDF]
A fragment-based screen against human immunodeficiency virus type 1 (HIV) integrase led to a number of compounds that bound to the lens epithelium derived growth factor (LEDGF) binding site of the integrase catalytic core domain.
Thomas S Peat +15 more
doaj +1 more source
Clinical use of HIV integrase inhibitors : a systematic review and meta-analysis [PDF]
Background: Optimal regimen choice of antiretroviral therapy is essential to achieve long-term clinical success. Integrase inhibitors have swiftly been adopted as part of current antiretroviral regimens.
A Talbot +59 more
core +8 more sources
HIV-1 Integrase: From Biology to Chemotherapeutics [PDF]
AIDS has claimed the lives of 25 million people worldwide, an additional 40 million people are HIV-infected and new cases are being diagnosed every year. Despite the fact that HAART has moved AIDS from the category of terminal diseases to that of treatable chronic illnesses, its long-term therapeutic success may be compromised by the development of ...
Zeinalipour-Loizidou, E. +7 more
openaire +4 more sources

