Metalloenzymes are central to a wide range of essential biological activities, including
nucleic acid modification, protein degradation, and many others. The role of metalloenzymes …

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 …

Dolutegravir is a second-generation integrase strand transfer inhibitor (INSTI) currently
under review by the US Food and Drug Administration for marketing approval. The in vitro …

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 …

Summary Background Dolutegravir (S/GSK1349572) is a new HIV-1 integrase inhibitor that
has antiviral activity with once daily, unboosted dosing. SPRING-1 is an ongoing study …

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 …

The integrase inhibitor (INI) dolutegravir (DTG; S/GSK1349572) has significant activity
against HIV-1 isolates with raltegravir (RAL)-and elvitegravir (ELV)-associated resistance …

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 …