Raltegravir (Isentress) is the first approved HIV integrase inhibitor. Agents in this class target a different viral enzyme compared with agents inhibiting reverse transcriptase and protease. A wide number of patients are currently susceptible to integrase inhibitors, including heavily antiretroviral-experienced patients harbouring drug-resistant viruses. The good tolerability and convenience o...

To design new chemotypes with enhanced potencies against the HIV integrase enzyme, 3D pharmacophore models were generated and QSAR study was carried out on 44 novel indole b-diketo acid derivatives and coumarin-based Inhibitors. A five-point pharmacophore with two hydrogen bond acceptors (A) and three aromatic rings (R) as pharmacophore features was developed by PHASE module of Schrodinger suit...

The retroviral integrase superfamily (RISF) comprises numerous important nucleic acid-processing enzymes, including transposases, integrases and various nucleases. These enzymes are involved in a wide range of processes such as transposition, replication and repair of DNA, homologous recombination, and RNA-mediated gene silencing. Two out of the four enzymes that are encoded by the human immuno...

Raltegravir is the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor; it targets the strand transfer step of HIV-1 integration. Clinical trials have demonstrated that raltegravir-containing regimens have potent antiretroviral activity and are well tolerated in HIV-1-infected individuals. In antiretroviral treatment-experienced persons with drug-resistant HIV infecti...

Background: The hyaluronidases are the enzymes hydrolyze β-1, 4 glycosidic linkage of hyaluronan. Hyaluronan is a polymer consisting of a repeating disaccharide unit found in cumulus ovuforus complex, semen liquid and other tissue. Addition to hydrolyzing the hyaluronan, hyaluronidase can penetrate through the cumulus cells layer that surrounds the oocyte, thus it terms spreading factor. Moreov...

objective: the aim of present study was cloning and expression of phic31 integrase cdna in a bacterial expression vector. thus, an intra molecular assay vector was applied to show in vitro activity of recombinant protein. materials and methods: in this experimental study, phic31 cdna was subcloned into a prokaryotic expression vector and transformed into e.coli bl21 (de3). recombinant phic31 in...

HIV-1 integrase is the viral enzyme responsible for the insertion of the viral DNA into the host cell chromosome. This process occurs through two distinct biochemical reactions: the 30-processing of the viral DNA and the transesterification reaction. Because experimental structural information on the reaction intermediate is not available, several molecular models have been developed. Unfortuna...

The virally encoded integrase protein carries out retroviral integration, which requires specific interactions with the two ends of the viral DNA, and also with host DNA that is the target of integration. We attached a photo-cross-linking agent to specific viral and target DNA sites to identify regions of the integrase polypeptide that are in close proximity to those substrate features in the a...

background: phic31 integrase is a dna site-specific recombinase integrates dna into the chromosomes between the two sites of attb and attp. several pseudo attps have been identified in mammalian genomes with critical features for long-term expression of transgene. in this manuscript, we report a novel intrinsic pseudo attp site named chol1 in the chinese hamster genome implementing an inverse p...