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Items: 1 to 20 of 124

1.

Multimode, cooperative mechanism of action of allosteric HIV-1 integrase inhibitors.

Kessl JJ, Jena N, Koh Y, Taskent-Sezgin H, Slaughter A, Feng L, de Silva S, Wu L, Le Grice SF, Engelman A, Fuchs JR, Kvaratskhelia M.

J Biol Chem. 2012 May 11;287(20):16801-11. doi: 10.1074/jbc.M112.354373. Epub 2012 Mar 21.

2.

Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation.

Jurado KA, Wang H, Slaughter A, Feng L, Kessl JJ, Koh Y, Wang W, Ballandras-Colas A, Patel PA, Fuchs JR, Kvaratskhelia M, Engelman A.

Proc Natl Acad Sci U S A. 2013 May 21;110(21):8690-5. doi: 10.1073/pnas.1300703110. Epub 2013 Apr 22.

3.

New class of HIV-1 integrase (IN) inhibitors with a dual mode of action.

Tsiang M, Jones GS, Niedziela-Majka A, Kan E, Lansdon EB, Huang W, Hung M, Samuel D, Novikov N, Xu Y, Mitchell M, Guo H, Babaoglu K, Liu X, Geleziunas R, Sakowicz R.

J Biol Chem. 2012 Jun 15;287(25):21189-203. doi: 10.1074/jbc.M112.347534. Epub 2012 Apr 25.

4.

Allosteric inhibition of human immunodeficiency virus integrase: late block during viral replication and abnormal multimerization involving specific protein domains.

Gupta K, Brady T, Dyer BM, Malani N, Hwang Y, Male F, Nolte RT, Wang L, Velthuisen E, Jeffrey J, Van Duyne GD, Bushman FD.

J Biol Chem. 2014 Jul 25;289(30):20477-88.

5.

The Competitive Interplay between Allosteric HIV-1 Integrase Inhibitor BI/D and LEDGF/p75 during the Early Stage of HIV-1 Replication Adversely Affects Inhibitor Potency.

Feng L, Dharmarajan V, Serrao E, Hoyte A, Larue RC, Slaughter A, Sharma A, Plumb MR, Kessl JJ, Fuchs JR, Bushman FD, Engelman AN, Griffin PR, Kvaratskhelia M.

ACS Chem Biol. 2016 May 20;11(5):1313-21. doi: 10.1021/acschembio.6b00167. Epub 2016 Mar 2.

6.

Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication.

Christ F, Voet A, Marchand A, Nicolet S, Desimmie BA, Marchand D, Bardiot D, Van der Veken NJ, Van Remoortel B, Strelkov SV, De Maeyer M, Chaltin P, Debyser Z.

Nat Chem Biol. 2010 Jun;6(6):442-8. doi: 10.1038/nchembio.370. Epub 2010 May 16.

PMID:
20473303
7.

The A128T resistance mutation reveals aberrant protein multimerization as the primary mechanism of action of allosteric HIV-1 integrase inhibitors.

Feng L, Sharma A, Slaughter A, Jena N, Koh Y, Shkriabai N, Larue RC, Patel PA, Mitsuya H, Kessl JJ, Engelman A, Fuchs JR, Kvaratskhelia M.

J Biol Chem. 2013 May 31;288(22):15813-20. doi: 10.1074/jbc.M112.443390. Epub 2013 Apr 24.

8.

LEDGF/p75-independent HIV-1 replication demonstrates a role for HRP-2 and remains sensitive to inhibition by LEDGINs.

Schrijvers R, De Rijck J, Demeulemeester J, Adachi N, Vets S, Ronen K, Christ F, Bushman FD, Debyser Z, Gijsbers R.

PLoS Pathog. 2012;8(3):e1002558. doi: 10.1371/journal.ppat.1002558. Epub 2012 Mar 1.

9.

Non-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cells.

Balakrishnan M, Yant SR, Tsai L, O'Sullivan C, Bam RA, Tsai A, Niedziela-Majka A, Stray KM, Sakowicz R, Cihlar T.

PLoS One. 2013 Sep 9;8(9):e74163. doi: 10.1371/journal.pone.0074163. eCollection 2013.

10.

Dual inhibition of HIV-1 replication by integrase-LEDGF allosteric inhibitors is predominant at the post-integration stage.

Le Rouzic E, Bonnard D, Chasset S, Bruneau JM, Chevreuil F, Le Strat F, Nguyen J, Beauvoir R, Amadori C, Brias J, Vomscheid S, Eiler S, Lévy N, Delelis O, Deprez E, Saïb A, Zamborlini A, Emiliani S, Ruff M, Ledoussal B, Moreau F, Benarous R.

Retrovirology. 2013 Nov 21;10:144. doi: 10.1186/1742-4690-10-144.

11.

Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV.

Hombrouck A, De Rijck J, Hendrix J, Vandekerckhove L, Voet A, De Maeyer M, Witvrouw M, Engelborghs Y, Christ F, Gijsbers R, Debyser Z.

PLoS Pathog. 2007 Mar;3(3):e47.

12.

Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization.

Christ F, Shaw S, Demeulemeester J, Desimmie BA, Marchand A, Butler S, Smets W, Chaltin P, Westby M, Debyser Z, Pickford C.

Antimicrob Agents Chemother. 2012 Aug;56(8):4365-74. doi: 10.1128/AAC.00717-12. Epub 2012 Jun 4.

13.

LEDGIN-mediated Inhibition of Integrase-LEDGF/p75 Interaction Reduces Reactivation of Residual Latent HIV.

Vranckx LS, Demeulemeester J, Saleh S, Boll A, Vansant G, Schrijvers R, Weydert C, Battivelli E, Verdin E, Cereseto A, Christ F, Gijsbers R, Debyser Z.

EBioMedicine. 2016 Jun;8:248-64. doi: 10.1016/j.ebiom.2016.04.039. Epub 2016 May 13.

14.

Contribution of host nucleoporin 62 in HIV-1 integrase chromatin association and viral DNA integration.

Ao Z, Jayappa KD, Wang B, Zheng Y, Wang X, Peng J, Yao X.

J Biol Chem. 2012 Mar 23;287(13):10544-55. doi: 10.1074/jbc.M111.317057. Epub 2012 Feb 3.

15.

Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodeficiency virus.

Vandekerckhove L, Christ F, Van Maele B, De Rijck J, Gijsbers R, Van den Haute C, Witvrouw M, Debyser Z.

J Virol. 2006 Feb;80(4):1886-96.

16.

Multimodal mechanism of action of allosteric HIV-1 integrase inhibitors.

Jurado KA, Engelman A.

Expert Rev Mol Med. 2013 Nov 26;15:e14. doi: 10.1017/erm.2013.15. Review.

17.

Integrase mutants defective for interaction with LEDGF/p75 are impaired in chromosome tethering and HIV-1 replication.

Emiliani S, Mousnier A, Busschots K, Maroun M, Van Maele B, Tempé D, Vandekerckhove L, Moisant F, Ben-Slama L, Witvrouw M, Christ F, Rain JC, Dargemont C, Debyser Z, Benarous R.

J Biol Chem. 2005 Jul 8;280(27):25517-23. Epub 2005 Apr 25.

18.

Discovery of novel 3-hydroxypicolinamides as selective inhibitors of HIV-1 integrase-LEDGF/p75 interaction.

Zhang FH, Debnath B, Xu ZL, Yang LM, Song LR, Zheng YT, Neamati N, Long YQ.

Eur J Med Chem. 2017 Jan 5;125:1051-1063. doi: 10.1016/j.ejmech.2016.10.045. Epub 2016 Oct 20.

PMID:
27810592
19.

Rational design of LEDGINs as first allosteric integrase inhibitors for the treatment of HIV infection.

Desimmie BA, Demeulemeester J, Christ F, Debyser Z.

Drug Discov Today Technol. 2013 Dec;10(4):e517-22. doi: 10.1016/j.ddtec.2012.10.002. Review.

PMID:
24451643
20.

Zinc finger endonuclease targeting PSIP1 inhibits HIV-1 integration.

Badia R, Pauls E, Riveira-Munoz E, Clotet B, Esté JA, Ballana E.

Antimicrob Agents Chemother. 2014 Aug;58(8):4318-27. doi: 10.1128/AAC.02690-14. Epub 2014 May 12.

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