Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells

DJ Hazuda, P Felock, M Witmer, A Wolfe, K Stillmock… - Science, 2000 - science.org
Integrase is essential for human immunodeficiency virus–type 1 (HIV-1) replication; however,
potent inhibition of the isolated enzyme in biochemical assays has not readily translated …

HIV-1 antiretroviral drug therapy

EJ Arts, DJ Hazuda - Cold Spring Harbor …, 2012 - perspectivesinmedicine.cshlp.org
The most significant advance in the medical management of HIV-1 infection has been the
treatment of patients with antiviral drugs, which can suppress HIV-1 replication to undetectable …

[PDF][PDF] Genome-scale RNAi screen for host factors required for HIV replication

…, JC Castle, E Stec, M Ferrer, B Strulovici, DJ Hazuda… - Cell host & …, 2008 - cell.com
Human immunodeficiency virus (HIV)-1 depends on the host cell machinery to support its
replication. To discover cellular factors associated with HIV-1 replication, we conducted a …

[HTML][HTML] Raltegravir with optimized background therapy for resistant HIV-1 infection

…, AR Meibohm, MD Miller, DJ Hazuda… - … England Journal of …, 2008 - Mass Medical Soc
Background Raltegravir (MK-0518) is an inhibitor of human immunodeficiency virus type 1 (HIV-1)
integrase active against HIV-1 susceptible or resistant to older antiretroviral drugs. …

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection

…, C Gardelli, O Gonzalez Paz, DJ Hazuda… - Journal of medicinal …, 2008 - ACS Publications
Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded
enzymes required for replication and therefore a rational target for chemotherapeutic …

Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes

…, S Young, J Vacca, DJ Hazuda - Proceedings of the …, 2002 - National Acad Sciences
The process of integrating the reverse-transcribed HIV-1 DNA into the host chromosomal
DNA is catalyzed by the virally encoded enzyme integrase (IN). Integration requires two metal-…

[HTML][HTML] Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection

…, AR Meibohm, MD Miller, DJ Hazuda… - … England Journal of …, 2008 - Mass Medical Soc
Background We evaluated the efficacy of raltegravir and the development of viral resistance
in two identical trials involving patients who were infected with human immunodeficiency …

[HTML][HTML] Activation of HIV transcription with short-course vorinostat in HIV-infected patients on suppressive antiretroviral therapy

…, BP Martin, E Sinclair, SG Deeks, DJ Hazuda… - PLoS …, 2014 - journals.plos.org
<p>Human immunodeficiency virus (HIV) persistence in latently infected resting memory
CD4+ T-cells is the major barrier to HIV cure. Cellular histone deacetylases (HDACs) are …

[HTML][HTML] Host cell factors in HIV replication: meta-analysis of genome-wide studies

…, G Cagney, TL Diamond, H Zhou, DJ Hazuda… - PLoS …, 2009 - journals.plos.org
We have analyzed host cell genes linked to HIV replication that were identified in nine
genome-wide studies, including three independent siRNA screens. Overlaps among the siRNA …

HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase

…, T Hamill, JL Cole, DJ Hazuda - Proceedings of the …, 2000 - National Acad Sciences
Diketo acids such as L-731,988 are potent inhibitors of HIV-1 integrase that inhibit integration
and viral replication in cells. These compounds exhibit the unique ability to inhibit the …