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Items: 1 to 20 of 149

1.

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
2.

The LEDGF/p75 integrase interaction, a novel target for anti-HIV therapy.

Christ F, Debyser Z.

Virology. 2013 Jan 5;435(1):102-9. doi: 10.1016/j.virol.2012.09.033. Review. Erratum in: Virology. 2013 Mar 30;438(1):50.

3.

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.

4.

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.

5.

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.

6.

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.

7.

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.

8.

TALEN knockout of the PSIP1 gene in human cells: analyses of HIV-1 replication and allosteric integrase inhibitor mechanism.

Fadel HJ, Morrison JH, Saenz DT, Fuchs JR, Kvaratskhelia M, Ekker SC, Poeschla EM.

J Virol. 2014 Sep 1;88(17):9704-17. doi: 10.1128/JVI.01397-14. Epub 2014 Jun 18.

9.
10.

Identification of the LEDGF/p75 binding site in HIV-1 integrase.

Busschots K, Voet A, De Maeyer M, Rain JC, Emiliani S, Benarous R, Desender L, Debyser Z, Christ F.

J Mol Biol. 2007 Feb 2;365(5):1480-92. Epub 2006 Nov 3.

PMID:
17137594
11.

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.

12.

Phage display-directed discovery of LEDGF/p75 binding cyclic peptide inhibitors of HIV replication.

Desimmie BA, Humbert M, Lescrinier E, Hendrix J, Vets S, Gijsbers R, Ruprecht RM, Dietrich U, Debyser Z, Christ F.

Mol Ther. 2012 Nov;20(11):2064-75. doi: 10.1038/mt.2012.132. Epub 2012 Jul 24.

13.

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.

14.

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.

15.

A new class of multimerization selective inhibitors of HIV-1 integrase.

Sharma A, Slaughter A, Jena N, Feng L, Kessl JJ, Fadel HJ, Malani N, Male F, Wu L, Poeschla E, Bushman FD, Fuchs JR, Kvaratskhelia M.

PLoS Pathog. 2014 May 29;10(5):e1004171. doi: 10.1371/journal.ppat.1004171. eCollection 2014 May.

16.

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.

17.

Implication of serine residues 271, 273, and 275 in the human immunodeficiency virus type 1 cofactor activity of lens epithelium-derived growth factor/p75.

Garcia-Rivera JA, Bueno MT, Morales E, Kugelman JR, Rodriguez DF, Llano M.

J Virol. 2010 Jan;84(2):740-52. doi: 10.1128/JVI.01043-09. Epub 2009 Nov 4.

18.

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.

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.

Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication.

De Rijck J, Vandekerckhove L, Gijsbers R, Hombrouck A, Hendrix J, Vercammen J, Engelborghs Y, Christ F, Debyser Z.

J Virol. 2006 Dec;80(23):11498-509. Epub 2006 Sep 20.

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