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The M50I polymorphic substitution in association with the R263K mutation in HIV-1 subtype B integrase increases drug resistance but does not restore viral replicative fitness.

Wares M, Mesplède T, Quashie PK, Osman N, Han Y, Wainberg MA.

Retrovirology. 2014 Jan 17;11:7. doi: 10.1186/1742-4690-11-7.


Characterization of the R263K mutation in HIV-1 integrase that confers low-level resistance to the second-generation integrase strand transfer inhibitor dolutegravir.

Quashie PK, Mesplède T, Han YS, Oliveira M, Singhroy DN, Fujiwara T, Underwood MR, Wainberg MA.

J Virol. 2012 Mar;86(5):2696-705. doi: 10.1128/JVI.06591-11. Epub 2011 Dec 28.


Effect of HIV-1 integrase resistance mutations when introduced into SIVmac239 on susceptibility to integrase strand transfer inhibitors.

Hassounah SA, Mesplède T, Quashie PK, Oliveira M, Sandstrom PA, Wainberg MA.

J Virol. 2014 Sep 1;88(17):9683-92. doi: 10.1128/JVI.00947-14. Epub 2014 Jun 11.


Viral fitness cost prevents HIV-1 from evading dolutegravir drug pressure.

Mesplède T, Quashie PK, Osman N, Han Y, Singhroy DN, Lie Y, Petropoulos CJ, Huang W, Wainberg MA.

Retrovirology. 2013 Feb 22;10:22. doi: 10.1186/1742-4690-10-22.


Impact of primary elvitegravir resistance-associated mutations in HIV-1 integrase on drug susceptibility and viral replication fitness.

Abram ME, Hluhanich RM, Goodman DD, Andreatta KN, Margot NA, Ye L, Niedziela-Majka A, Barnes TL, Novikov N, Chen X, Svarovskaia ES, McColl DJ, White KL, Miller MD.

Antimicrob Agents Chemother. 2013 Jun;57(6):2654-63. doi: 10.1128/AAC.02568-12. Epub 2013 Mar 25.


Addition of E138K to R263K in HIV integrase increases resistance to dolutegravir, but fails to restore activity of the HIV integrase enzyme and viral replication capacity.

Mesplède T, Osman N, Wares M, Quashie PK, Hassounah S, Anstett K, Han Y, Singhroy DN, Wainberg MA.

J Antimicrob Chemother. 2014 Oct;69(10):2733-40. doi: 10.1093/jac/dku199. Epub 2014 Jun 10.


Genetic barrier to the development of resistance to integrase inhibitors in HIV-1 subtypes CRF01_AE and B.

Nguyen HL, Ruxrungtham K, Delaugerre C.

Intervirology. 2012;55(4):287-95. doi: 10.1159/000336658. Epub 2012 Mar 23.


Biochemical analysis of the role of G118R-linked dolutegravir drug resistance substitutions in HIV-1 integrase.

Quashie PK, Mesplède T, Han YS, Veres T, Osman N, Hassounah S, Sloan RD, Xu HT, Wainberg MA.

Antimicrob Agents Chemother. 2013 Dec;57(12):6223-35. doi: 10.1128/AAC.01835-13. Epub 2013 Sep 30. Erratum in: Antimicrob Agents Chemother. 2014 Jan;58(1):633.


Resistance to HIV integrase inhibitors.

Mesplède T, Quashie PK, Wainberg MA.

Curr Opin HIV AIDS. 2012 Sep;7(5):401-8. doi: 10.1097/COH.0b013e328356db89. Review.


The R263K mutation in HIV integrase that is selected by dolutegravir may actually prevent clinically relevant resistance to this compound.

Wainberg M, Anstett K, Mesplede T, Quashie P, Han Y, Oliveira M.

J Int AIDS Soc. 2014 Nov 2;17(4 Suppl 3):19518. doi: 10.7448/IAS.17.4.19518. eCollection 2014.


Resistance mutations against dolutegravir in HIV integrase impair the emergence of resistance against reverse transcriptase inhibitors.

Oliveira M, Mesplède T, Quashie PK, Moïsi D, Wainberg MA.

AIDS. 2014 Mar 27;28(6):813-9. doi: 10.1097/QAD.0000000000000199.


Resistance mutations outside the integrase coding region have an effect on human immunodeficiency virus replicative fitness but do not affect its susceptibility to integrase strand transfer inhibitors.

Weber J, Rose JD, Vazquez AC, Winner D, Margot N, McColl DJ, Miller MD, Quiñones-Mateu ME.

PLoS One. 2013 Jun 11;8(6):e65631. doi: 10.1371/journal.pone.0065631. Print 2013.


The development of novel HIV integrase inhibitors and the problem of drug resistance.

Wainberg MA, Mesplède T, Quashie PK.

Curr Opin Virol. 2012 Oct;2(5):656-62. doi: 10.1016/j.coviro.2012.08.007. Epub 2012 Sep 16. Review.


HIV-1 group O integrase displays lower susceptibility to raltegravir and has a different mutational pathway for resistance than HIV-1 group M.

Depatureaux A, Mesplède T, Quashie P, Oliveira M, Moisi D, Brenner B, Wainberg M.

J Int AIDS Soc. 2014 Nov 2;17(4 Suppl 3):19738. doi: 10.7448/IAS.17.4.19738. eCollection 2014.


Dolutegravir (S/GSK1349572) exhibits significantly slower dissociation than raltegravir and elvitegravir from wild-type and integrase inhibitor-resistant HIV-1 integrase-DNA complexes.

Hightower KE, Wang R, Deanda F, Johns BA, Weaver K, Shen Y, Tomberlin GH, Carter HL 3rd, Broderick T, Sigethy S, Seki T, Kobayashi M, Underwood MR.

Antimicrob Agents Chemother. 2011 Oct;55(10):4552-9. doi: 10.1128/AAC.00157-11. Epub 2011 Aug 1.


Identification of novel mutations responsible for resistance to MK-2048, a second-generation HIV-1 integrase inhibitor.

Bar-Magen T, Sloan RD, Donahue DA, Kuhl BD, Zabeida A, Xu H, Oliveira M, Hazuda DJ, Wainberg MA.

J Virol. 2010 Sep;84(18):9210-6. doi: 10.1128/JVI.01164-10. Epub 2010 Jul 7.


Emerging patterns and implications of HIV-1 integrase inhibitor resistance.

Geretti AM, Armenia D, Ceccherini-Silberstein F.

Curr Opin Infect Dis. 2012 Dec;25(6):677-86. doi: 10.1097/QCO.0b013e32835a1de7. Review.


Mutation Q95K enhances N155H-mediated integrase inhibitor resistance and improves viral replication capacity.

Fun A, Van Baelen K, van Lelyveld SF, Schipper PJ, Stuyver LJ, Wensing AM, Nijhuis M.

J Antimicrob Chemother. 2010 Nov;65(11):2300-4. doi: 10.1093/jac/dkq319. Epub 2010 Aug 24.


Characterization and structural analysis of HIV-1 integrase conservation.

Ceccherini-Silberstein F, Malet I, D'Arrigo R, Antinori A, Marcelin AG, Perno CF.

AIDS Rev. 2009 Jan-Mar;11(1):17-29. Review.


The HIV-1 integrase G118R mutation confers raltegravir resistance to the CRF02_AG HIV-1 subtype.

Malet I, Fourati S, Charpentier C, Morand-Joubert L, Armenia D, Wirden M, Sayon S, Van Houtte M, Ceccherini-Silberstein F, Brun-Vézinet F, Perno CF, Descamps D, Capt A, Calvez V, Marcelin AG.

J Antimicrob Chemother. 2011 Dec;66(12):2827-30. doi: 10.1093/jac/dkr389. Epub 2011 Sep 19.

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