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In vitro analysis of the susceptibility of HIV-1 subtype A and CRF01_AE integrases to raltegravir.
| dc.rights.license | open | en_US |
| hal.structure.identifier | Microbiologie Fondamentale et Pathogénicité [MFP] | |
| dc.contributor.author | BELLECAVE, Pantxika | |
| hal.structure.identifier | Microbiologie Fondamentale et Pathogénicité [MFP] | |
| dc.contributor.author | MALATO, Laurent | |
| hal.structure.identifier | Microbiologie Fondamentale et Pathogénicité [MFP] | |
| dc.contributor.author | CALMELS, Christina | |
| dc.contributor.author | REIGADAS, Sandrine | |
| hal.structure.identifier | Microbiologie Fondamentale et Pathogénicité [MFP] | |
| dc.contributor.author | PARISSI, Vincent | |
| hal.structure.identifier | Microbiologie Fondamentale et Pathogénicité [MFP] | |
| dc.contributor.author | ANDREOLA, Marie-Line | |
| hal.structure.identifier | Microbiologie Fondamentale et Pathogénicité [MFP] | |
| dc.contributor.author | FLEURY, Hervé | |
| dc.date.accessioned | 2024-11-05T13:22:07Z | |
| dc.date.available | 2024-11-05T13:22:07Z | |
| dc.date.issued | 2014-08-01 | |
| dc.identifier.issn | 1872-7913 | en_US |
| dc.identifier.uri | https://oskar-bordeaux.fr/handle/20.500.12278/203129 | |
| dc.description.abstractEn | The antiviral efficacy of raltegravir (RAL) has been proven against human immunodeficiency virus type 1 (HIV-1) subtypes B and C but remained to be determined against other subtypes. Therefore, the enzymatic activities as well as RAL resistance of HIV-1 subtype A and CRF01_AE integrases (INs) were investigated. Previously published subtype A and CRF01_AE IN sequences from RAL-naïve patients were aligned to generate consensus sequences for both IN subtypes. Subtype A and CRF01_AE INs encoded by these consensus sequences as well as the corresponding enzymes harbouring the N155H resistance mutation were expressed and purified. Enzymatic activities of subtype A and CRF01_AE INs were analysed with regard to typical 3'-end processing (3'-P) and strand transfer (ST) activities both in the presence and absence of RAL and were compared with subtype B IN as well as with the corresponding INs harbouring the N155H resistance mutation. Subtypes B, A and CRF01_AE INs showed similar 3'-P and ST activities. In the presence of RAL, the three wild-type INs exhibited ST activity IC50 values (50% inhibitory concentrations) of 86.3 ± 32.5, 158.3 ± 99.0 and 100.0 ± 65.7 nM, respectively. Analysis of 3'-P activity in the presence of RAL revealed IC(50) > 10 μM for all three enzymes. The three INs harbouring the N155H mutation presented in vitro low but similar resistance levels to RAL. In conclusion, INs from HIV-1 subtypes B, A and CRF01_AE showed similar responses to RAL in vitro, suggesting the potency of this antiretroviral drug to treat HIV-1 subtype A- and CRF01_AE-infected patients. | |
| dc.language.iso | EN | en_US |
| dc.subject.en | Anti-HIV Agents | |
| dc.subject.en | Cloning | |
| dc.subject.en | Molecular | |
| dc.subject.en | Gene Expression | |
| dc.subject.en | Genotype | |
| dc.subject.en | HIV Integrase | |
| dc.subject.en | HIV-1 | |
| dc.subject.en | Humans | |
| dc.subject.en | Inhibitory Concentration 50 | |
| dc.subject.en | Microbial Sensitivity Tests | |
| dc.subject.en | Mutant Proteins | |
| dc.subject.en | Pyrrolidinones | |
| dc.subject.en | Raltegravir Potassium | |
| dc.title.en | In vitro analysis of the susceptibility of HIV-1 subtype A and CRF01_AE integrases to raltegravir. | |
| dc.title.alternative | Int J Antimicrob Agents | en_US |
| dc.type | Article de revue | en_US |
| dc.identifier.doi | 10.1016/j.ijantimicag.2014.04.013 | en_US |
| dc.subject.hal | Sciences du Vivant [q-bio]/Microbiologie et Parasitologie | en_US |
| dc.identifier.pubmed | 24935032 | en_US |
| bordeaux.journal | International Journal of Antimicrobial Agents | en_US |
| bordeaux.page | 168-72 | en_US |
| bordeaux.volume | 44 | en_US |
| bordeaux.hal.laboratories | MFP (Laboratoire Microbiologie Fondamentale et Pathogénicité) - UMR 5234 | en_US |
| bordeaux.issue | 2 | en_US |
| bordeaux.institution | CNRS | en_US |
| bordeaux.peerReviewed | oui | en_US |
| bordeaux.inpress | non | en_US |
| bordeaux.import.source | pubmed | |
| hal.popular | non | en_US |
| hal.audience | Internationale | en_US |
| hal.export | false | |
| workflow.import.source | pubmed | |
| dc.rights.cc | Pas de Licence CC | en_US |
| bordeaux.COinS | ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=International%20Journal%20of%20Antimicrobial%20Agents&rft.date=2014-08-01&rft.volume=44&rft.issue=2&rft.spage=168-72&rft.epage=168-72&rft.eissn=1872-7913&rft.issn=1872-7913&rft.au=BELLECAVE,%20Pantxika&MALATO,%20Laurent&CALMELS,%20Christina&REIGADAS,%20Sandrine&PARISSI,%20Vincent&rft.genre=article |
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