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Block-and-lock strategies to cure HIV infection
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 …
cells inducing a viral rebound upon treatment interruption. Hence, the latent reservoir is …
Retroviral DNA integration
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 …
step of retroviral replication. This enzymatic process is catalyzed by the virus-encoded …
Structural and mechanistic bases for a potent HIV-1 capsid inhibitor
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 …
acting antiretroviral therapy. We found that GS-6207 inhibits HIV-1 by stabilizing and thereby …
[HTML][HTML] HIV-1 maturation: Lessons learned from inhibitors
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 …
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?
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 …
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
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 …
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
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) …
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
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 …
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
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 …
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 …
(IN) inhibitors that are structurally distinct from IN strand transfer inhibitors but analogous to …