Block-and-lock strategies to cure HIV infection

G Vansant, A Bruggemans, J Janssens, Z Debyser - Viruses, 2020 - mdpi.com
Today HIV infection cannot be cured due to the presence of a reservoir of latently infected
cells inducing a viral rebound upon treatment interruption. Hence, the latent reservoir is …

Retroviral DNA integration

P Lesbats, AN Engelman, P Cherepanov - Chemical reviews, 2016 - ACS Publications
The integration of a DNA copy of the viral RNA genome into host chromatin is the defining
step of retroviral replication. This enzymatic process is catalyzed by the virus-encoded …

[HTML][HTML] Establishment of latent HIV-1 reservoirs: what do we really know?

J Vanhamel, A Bruggemans, Z Debyser - Journal of virus eradication, 2019 - Elsevier
Despite our ability to suppress HIV-1 replication indefinitely in people on optimal combined
antiretroviral therapy (cART), HIV-1 persists as a stably integrated and replication-competent …

HIV-1 latency in monocytes/macrophages

A Kumar, W Abbas, G Herbein - Viruses, 2014 - mdpi.com
Human immunodeficiency virus type 1 (HIV-1) targets CD4+ T cells and cells of the
monocyte/macrophage lineage. HIV pathogenesis is characterized by the depletion of T …

Molecular basis of human immunodeficiency virus type 1 drug resistance: overview and recent developments

L Menéndez-Arias - Antiviral research, 2013 - Elsevier
The introduction of potent combination therapies in the mid-90s had a tremendous effect on
AIDS mortality. However, drug resistance has been a major factor contributing to …

Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation

KA Jurado, H Wang, A Slaughter… - Proceedings of the …, 2013 - National Acad Sciences
Integration is essential for HIV-1 replication, and the viral integrase (IN) protein is an
important therapeutic target. Allosteric IN inhibitors (ALLINIs) that engage the IN dimer …

Discovery of BI 224436, a noncatalytic site integrase inhibitor (NCINI) of HIV-1

LD Fader, E Malenfant, M Parisien… - ACS medicinal …, 2014 - ACS Publications
An assay recapitulating the 3′ processing activity of HIV-1 integrase (IN) was used to
screen the Boehringer Ingelheim compound collection. Hit-to-lead and lead optimization …

The chromatin landscape at the HIV-1 provirus integration site determines viral expression

G Vansant, HC Chen, E Zorita, K Trejbalová… - Nucleic acids …, 2020 - academic.oup.com
HIV-1 persists lifelong in memory cells of the immune system as latent provirus that
rebounds upon treatment interruption. Therefore, the latent reservoir is the main target for an …

Insights into persistent HIV-1 infection and functional cure: novel capabilities and strategies

TM Ta, S Malik, EM Anderson, AD Jones… - Frontiers in …, 2022 - frontiersin.org
Although HIV-1 replication can be efficiently suppressed to undetectable levels in peripheral
blood by combination antiretroviral therapy (cART), lifelong medication is still required in …

Non-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cells

M Balakrishnan, SR Yant, L Tsai, C O'Sullivan… - PloS one, 2013 - journals.plos.org
HIV-1 integrase (IN) is the target for two classes of antiretrovirals: i) the integrase strand-
transfer inhibitors (INSTIs) and ii) the non-catalytic site integrase inhibitors (NCINIs). NCINIs …