Abstract Merck's MK-0518, known as raltegravir, has recently become the first FDA-
approved HIV-1 integrase (IN) inhibitor and has since risen to blockbuster drug status. Much …

Quinolones are among the most common frameworks present in the bioactive molecules
and hence represent an attractive starting point for the design of combinatorial libraries …

Background Two inhibitors of the HIV-1 integrase enzyme (INIs) are in late stage clinical
development. To date, approximately 42 mutations within the HIV-1 integrase (IN) gene …

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 …

Two decades of intensive research efforts have led to the discovery of a large number of HIV-
1 integrase (IN) inhibitors. Recently, the United States Food and Drug Administration (US …

Metal-activated enzymes are important targets in drug discovery in general and for antivirals
in particular. Such proteins contain one or more metal ion cofactors, prevalently located in …

The first integrase inhibitor licensed to treat HIV-1 infection was approved in late 2007, more
than a decade after the introduction of the first inhibitors of the HIV-1 reverse transcriptase …

Several small molecule drugs that bind to the host CCR5 co-receptor and prevent viral entry
have been developed for the treatment of HIV-1 infection. The innate variability found in HIV …

HIV-1 integrase (IN) has been validated as an attractive target for the treatment of HIV/AIDS.
Several studies have confirmed that the metal binding function is a crucial feature in many of …

HIV integrase became an important target for drug development more than twenty years
ago. However, progress has been hampered by the lack of assays suitable for high …