Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137)
K Shimura, E Kodama, Y Sakagami… - Journal of …, 2008 - Am Soc Microbiol
Integrase (IN), an essential enzyme of human immunodeficiency virus (HIV), is an attractive
antiretroviral drug target. The antiviral activity and resistance profile in vitro of a novel IN …
antiretroviral drug target. The antiviral activity and resistance profile in vitro of a novel IN …
HIV‐1 integrase inhibitors: 2005–2006 update
Abstract HIV‐1 integrase (IN) catalyzes the integration of proviral DNA into the host genome,
an essential step for viral replication. Inhibition of IN catalytic activity provides an attractive …
an essential step for viral replication. Inhibition of IN catalytic activity provides an attractive …
Mechanisms and inhibition of HIV integration
C Marchand, AA Johnson, E Semenova… - Drug Discovery Today …, 2006 - Elsevier
HIV integrase (IN) is required for viral replication and a rationale target for antiretroviral
therapies. Integrase inhibitors are potentially complementary to current treatments. This …
therapies. Integrase inhibitors are potentially complementary to current treatments. This …
In-Silicodocking of HIV-1 integrase inhibitors reveals a novel drug type acting on an enzyme/DNA reaction intermediate
A Savarino - Retrovirology, 2007 - Springer
Abstract Background HIV-1 integrase (IN) is an emerging drug target, as IN strand transfer
inhibitors (INSTIs) are proving potent antiretroviral agents in clinical trials. One credible …
inhibitors (INSTIs) are proving potent antiretroviral agents in clinical trials. One credible …
The catalytic mechanism of HIV-1 integrase for DNA 3′-end processing established by QM/MM calculations
The development of HIV-1 integrase (INT) inhibitors has been hampered by incomplete
structural and mechanistic information. Despite the efforts made to overcome these …
structural and mechanistic information. Despite the efforts made to overcome these …
Induced‐fit docking approach provides insight into the binding mode and mechanism of action of HIV‐1 integrase inhibitors
A three‐dimensional model of a complex between HIV‐1 integrase (IN), viral DNA, and
metal ions that we recently built was used as a target for a docking method (induced‐fit …
metal ions that we recently built was used as a target for a docking method (induced‐fit …
A dynamic model of HIV integrase inhibition and drug resistance
Human immunodeficiency virus type 1 (HIV-1) integrase is one of three virally encoded
enzymes essential for replication and, therefore, a rational choice as a drug target for the …
enzymes essential for replication and, therefore, a rational choice as a drug target for the …
HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation
L De Luca, S De Grazia, S Ferro, R Gitto… - European journal of …, 2011 - Elsevier
This study is focused on a new series of benzylindole derivatives with various substituents at
the benzene-fused ring, suggested by our 3D pharmacophore model developed for HIV-1 …
the benzene-fused ring, suggested by our 3D pharmacophore model developed for HIV-1 …
Subunit-specific protein footprinting reveals significant structural rearrangements and a role for N-terminal Lys-14 of HIV-1 Integrase during viral DNA binding
Z Zhao, CJ McKee, JJ Kessl, WL Santos… - Journal of Biological …, 2008 - ASBMB
To identify functional contacts between HIV-1 integrase (IN) and its viral DNA substrate, we
devised a new experimental strategy combining the following two methodologies. First …
devised a new experimental strategy combining the following two methodologies. First …
Posttranslational acetylation of the human immunodeficiency virus type 1 integrase carboxyl-terminal domain is dispensable for viral replication
M Topper, Y Luo, M Zhadina, K Mohammed… - Journal of …, 2007 - Am Soc Microbiol
ABSTRACT A recent report sought to demonstrate that acetylation of specific lysines within
integrase (IN) by the histone acetyltransferase (HAT) p300 regulates human …
integrase (IN) by the histone acetyltransferase (HAT) p300 regulates human …