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 …
treatment of patients with antiviral drugs, which can suppress HIV-1 replication to …
The structural biology of HIV-1: mechanistic and therapeutic insights
A Engelman, P Cherepanov - Nature Reviews Microbiology, 2012 - nature.com
Three-dimensional molecular structures can provide detailed information on biological
mechanisms and, for cases in which the molecular function affects human health, can …
mechanisms and, for cases in which the molecular function affects human health, can …
Structure and function of retroviral integrase
GN Maertens, AN Engelman… - Nature Reviews …, 2022 - nature.com
A hallmark of retroviral replication is establishment of the proviral state, wherein a DNA copy
of the viral RNA genome is stably incorporated into a host cell chromosome. Integrase is the …
of the viral RNA genome is stably incorporated into a host cell chromosome. Integrase is the …
Metal–ligand interactions in drug design
The fast-growing body of experimental data on metalloenzymes and organometallic
compounds is fostering the exploitation of metal–ligand interactions for the design of new …
compounds is fostering the exploitation of metal–ligand interactions for the design of new …
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 …
step of retroviral replication. This enzymatic process is catalyzed by the virus-encoded …
HIV drug resistance against strand transfer integrase inhibitors
K Anstett, B Brenner, T Mesplede, MA Wainberg - Retrovirology, 2017 - Springer
Integrase strand transfer inhibitors (INSTIs) are the newest class of antiretroviral drugs to be
approved for treatment and act by inhibiting the essential HIV protein integrase from …
approved for treatment and act by inhibiting the essential HIV protein integrase from …
Cryo-EM structures and atomic model of the HIV-1 strand transfer complex intasome
Like all retroviruses, HIV-1 irreversibly inserts a viral DNA (vDNA) copy of its RNA genome
into host target DNA (tDNA). The intasome, a higher-order nucleoprotein complex composed …
into host target DNA (tDNA). The intasome, a higher-order nucleoprotein complex composed …
Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572)
S Hare, SJ Smith, M Métifiot, A Jaxa-Chamiec… - Molecular …, 2011 - ASPET
Raltegravir (RAL) and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs)
efficiently block viral replication in vitro and suppress viremia in patients. These small …
efficiently block viral replication in vitro and suppress viremia in patients. These small …
Interfacial inhibitors: targeting macromolecular complexes
Y Pommier, C Marchand - Nature reviews Drug discovery, 2012 - nature.com
Interfacial inhibitors belong to a broad class of natural products and synthetic drugs that are
commonly used to treat cancers as well as bacterial and HIV infections. They bind …
commonly used to treat cancers as well as bacterial and HIV infections. They bind …
Dolutegravir (S/GSK1349572) exhibits significantly slower dissociation than raltegravir and elvitegravir from wild-type and integrase inhibitor-resistant HIV-1 integrase …
KE Hightower, R Wang, F DeAnda… - Antimicrobial agents …, 2011 - Am Soc Microbiol
The integrase inhibitor (INI) dolutegravir (DTG; S/GSK1349572) has significant activity
against HIV-1 isolates with raltegravir (RAL)-and elvitegravir (ELV)-associated resistance …
against HIV-1 isolates with raltegravir (RAL)-and elvitegravir (ELV)-associated resistance …