Integrase and integration: biochemical activities of HIV-1 integrase

O Delelis, K Carayon, A Saïb, E Deprez, JF Mouscadet - Retrovirology, 2008 - Springer
Integration of retroviral DNA is an obligatory step of retrovirus replication because proviral
DNA is the template for productive infection. Integrase, a retroviral enzyme, catalyses …

Resistance to integrase inhibitors

M Métifiot, C Marchand, K Maddali, Y Pommier - Viruses, 2010 - mdpi.com
Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency
virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced …

Structure-based modeling of the functional HIV-1 intasome and its inhibition

L Krishnan, X Li, HL Naraharisetty… - Proceedings of the …, 2010 - National Acad Sciences
The intasome is the basic recombination unit of retroviral integration, comprising the
integrase protein and the ends of the viral DNA made by reverse transcription. Clinical …

Relationship between the oligomeric status of HIV-1 integrase on DNA and enzymatic activity

E Guiot, K Carayon, O Delelis, F Simon, P Tauc… - Journal of Biological …, 2006 - ASBMB
The 3′-processing of the extremities of viral DNA is the first of two reactions catalyzed by
HIV-1 integrase (IN). High order IN multimers (tetramers) are required for complete …

Dolutegravir interactions with HIV-1 integrase-DNA: structural rationale for drug resistance and dissociation kinetics

F DeAnda, KE Hightower, RT Nolte, K Hattori… - PLoS …, 2013 - journals.plos.org
Signature HIV-1 integrase mutations associated with clinical raltegravir resistance involve 1
of 3 primary genetic pathways, Y143C/R, Q148H/K/R and N155H, the latter 2 of which confer …

HIV‐1 integrase inhibitors: 2005–2006 update

R Dayam, R Gundla, LQ Al‐Mawsawi… - Medicinal Research …, 2008 - Wiley Online Library
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 …

Structural basis for HIV‐1 DNA integration in the human genome, role of the LEDGF/P75 cofactor

F Michel, C Crucifix, F Granger, S Eiler… - The EMBO …, 2009 - embopress.org
Integration of the human immunodeficiency virus (HIV‐1) cDNA into the human genome is
catalysed by integrase. Several studies have shown the importance of the interaction of …

Resistance to HIV-1 integrase inhibitors: a structural perspective

JF Mouscadet, O Delelis, AG Marcelin… - Drug Resistance …, 2010 - Elsevier
Strand-transfer inhibitors, of which raltegravir, elvitegravir and S/GSK1349572, is a new
class of antiretrovirals that inhibit HIV integrase-catalyzed insertion of the HIV-1 genome into …

Impact of Y143 HIV-1 Integrase Mutations on Resistance to Raltegravir In Vitro and In Vivo

O Delelis, S Thierry, F Subra, F Simon… - Antimicrobial agents …, 2010 - Am Soc Microbiol
ABSTRACT Integrase (IN), the HIV-1 enzyme responsible for the integration of the viral
genome into the chromosomes of infected cells, is the target of the recently approved …

The structure of the bacterial oxidoreductase enzyme DsbA in complex with a peptide reveals a basis for substrate specificity in the catalytic cycle of DsbA enzymes

JJ Paxman, NA Borg, J Horne, PE Thompson… - Journal of biological …, 2009 - ASBMB
Oxidative protein folding in Gram-negative bacteria results in the formation of disulfide
bonds between pairs of cysteine residues. This is a multistep process in which the dithiol …