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 …

Structural and mechanistic bases for a potent HIV-1 capsid inhibitor

SM Bester, G Wei, H Zhao, D Adu-Ampratwum, N Iqbal… - Science, 2020‏ - science.org
The potent HIV-1 capsid inhibitor GS-6207 is an investigational principal component of long-
acting antiretroviral therapy. We found that GS-6207 inhibits HIV-1 by stabilizing and thereby …

[HTML][HTML] HIV-1 maturation: Lessons learned from inhibitors

AB Kleinpeter, EO Freed - Viruses, 2020‏ - mdpi.com
Since the emergence of HIV and AIDS in the early 1980s, the development of safe and
effective therapies has accompanied a massive increase in our understanding of the …

[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 …

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

KA Jurado, H Wang, A Slaughter, L Feng… - Proceedings of the …, 2013‏ - pnas.org
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 …

[HTML][HTML] HIV-1 integrase binds the viral RNA genome and is essential during virion morphogenesis

JJ Kessl, SB Kutluay, D Townsend, S Rebensburg… - Cell, 2016‏ - cell.com
While an essential role of HIV-1 integrase (IN) for integration of viral cDNA into human
chromosome is established, studies with IN mutants and allosteric IN inhibitors (ALLINIs) …

Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization

F Christ, S Shaw, J Demeulemeester… - Antimicrobial agents …, 2012‏ - journals.asm.org
Targeting the HIV integrase (HIV IN) is a clinically validated approach for designing novel
anti-HIV therapies. We have previously described the discovery of a novel class of …

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 …

[HTML][HTML] New class of HIV-1 integrase (IN) inhibitors with a dual mode of action

M Tsiang, GS Jones, A Niedziela-Majka, E Kan… - Journal of Biological …, 2012‏ - Elsevier
tert-Butoxy-(4-phenyl-quinolin-3-yl)-acetic acids (tBPQA) are a new class of HIV-1 integrase
(IN) inhibitors that are structurally distinct from IN strand transfer inhibitors but analogous to …