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 …

Three-dimensional molecular structures can provide detailed information on biological
mechanisms and, for cases in which the molecular function affects human health, can …

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 …

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 …

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 …

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 …

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 …

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 …

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 …

We report herein the discovery of the human immunodeficiency virus type-1 (HIV-1)
integrase inhibitors dolutegravir (S/GSK1349572)(3) and S/GSK1265744 (4). These drugs …