Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 268

1.

Capsid labelled HIV to investigate the role of capsid during nuclear import and integration.

Zurnic Bönisch I, Dirix L, Lemmens V, Borrenberghs D, De Wit F, Vernaillen F, Rocha S, Christ F, Hendrix J, Hofkens J, Debyser Z.

J Virol. 2020 Jan 15. pii: JVI.01024-19. doi: 10.1128/JVI.01024-19. [Epub ahead of print]

PMID:
31941774
2.

The mutation of Transportin 3 gene that causes limb girdle muscular dystrophy 1F induces protection against HIV-1 infection.

Rodríguez-Mora S, De Wit F, García-Perez J, Bermejo M, López-Huertas MR, Mateos E, Martí P, Rocha S, Vigón L, Christ F, Debyser Z, Vílchez JJ, Coiras M, Alcamí J.

PLoS Pathog. 2019 Aug 29;15(8):e1007958. doi: 10.1371/journal.ppat.1007958. eCollection 2019 Aug.

3.

Identification of Novel 3-Hydroxy-pyran-4-One Derivatives as Potent HIV-1 Integrase Inhibitors Using in silico Structure-Based Combinatorial Library Design Approach.

Sirous H, Chemi G, Gemma S, Butini S, Debyser Z, Christ F, Saghaie L, Brogi S, Fassihi A, Campiani G, Brindisi M.

Front Chem. 2019 Aug 13;7:574. doi: 10.3389/fchem.2019.00574. eCollection 2019.

4.

Synthesis and Anti-HIV Profile of a Novel Tetrahydroindazolylbenzamide Derivative Obtained by Oxazolone Chemistry.

Scala A, Piperno A, Micale N, Christ F, Debyser Z.

ACS Med Chem Lett. 2018 Dec 15;10(4):398-401. doi: 10.1021/acsmedchemlett.8b00511. eCollection 2019 Apr 11.

5.

Impact of LEDGIN treatment during virus production on residual HIV-1 transcription.

Vansant G, Vranckx LS, Zurnic I, Van Looveren D, Van de Velde P, Nobles C, Gijsbers R, Christ F, Debyser Z.

Retrovirology. 2019 Apr 2;16(1):8. doi: 10.1186/s12977-019-0472-3.

6.

Insight in HIV Integration Site Selection Provides a Block-and-Lock Strategy for a Functional Cure of HIV Infection.

Debyser Z, Vansant G, Bruggemans A, Janssens J, Christ F.

Viruses. 2018 Dec 26;11(1). pii: E12. doi: 10.3390/v11010012. Review.

7.

Synthesis, Molecular Modelling and Biological Studies of 3-hydroxypyrane- 4-one and 3-hydroxy-pyridine-4-one Derivatives as HIV-1 Integrase Inhibitors.

Sirous H, Fassihi A, Brogi S, Campiani G, Christ F, Debyser Z, Gemma S, Butini S, Chemi G, Grillo A, Zabihollahi R, Aghasadeghi MR, Saghaie L, Memarian HR.

Med Chem. 2019;15(7):755-770. doi: 10.2174/1573406415666181219113225.

PMID:
30569867
8.

Affinity switching of the LEDGF/p75 IBD interactome is governed by kinase-dependent phosphorylation.

Sharma S, Čermáková K, De Rijck J, Demeulemeester J, Fábry M, El Ashkar S, Van Belle S, Lepšík M, Tesina P, Duchoslav V, Novák P, Hubálek M, Srb P, Christ F, Řezáčová P, Hodges HC, Debyser Z, Veverka V.

Proc Natl Acad Sci U S A. 2018 Jul 24;115(30):E7053-E7062. doi: 10.1073/pnas.1803909115. Epub 2018 Jul 11.

9.

Inhibitors of the integrase-transportin-SR2 interaction block HIV nuclear import.

Demeulemeester J, Blokken J, De Houwer S, Dirix L, Klaassen H, Marchand A, Chaltin P, Christ F, Debyser Z.

Retrovirology. 2018 Jan 12;15(1):5. doi: 10.1186/s12977-018-0389-2.

10.

Protein-protein and protein-chromatin interactions of LEDGF/p75 as novel drug targets.

Blokken J, De Rijck J, Christ F, Debyser Z.

Drug Discov Today Technol. 2017 Jun;24:25-31. doi: 10.1016/j.ddtec.2017.11.002. Epub 2017 Nov 23. Review.

PMID:
29233296
11.

LEDGF/p75 is dispensable for hematopoiesis but essential for MLL-rearranged leukemogenesis.

El Ashkar S, Schwaller J, Pieters T, Goossens S, Demeulemeester J, Christ F, Van Belle S, Juge S, Boeckx N, Engelman A, Van Vlierberghe P, Debyser Z, De Rijck J.

Blood. 2018 Jan 4;131(1):95-107. doi: 10.1182/blood-2017-05-786962. Epub 2017 Oct 30.

12.

N-terminal half of transportin SR2 interacts with HIV integrase.

Tsirkone VG, Blokken J, De Wit F, Breemans J, De Houwer S, Debyser Z, Christ F, Strelkov SV.

J Biol Chem. 2017 Jun 9;292(23):9699-9710. doi: 10.1074/jbc.M117.777029. Epub 2017 Mar 29.

13.

Insight into HIV-2 latency may disclose strategies for a cure for HIV-1 infection.

Saleh S, Vranckx L, Gijsbers R, Christ F, Debyser Z.

J Virus Erad. 2017 Jan 1;3(1):7-14.

14.

Dynamic Oligomerization of Integrase Orchestrates HIV Nuclear Entry.

Borrenberghs D, Dirix L, De Wit F, Rocha S, Blokken J, De Houwer S, Gijsbers R, Christ F, Hofkens J, Hendrix J, Debyser Z.

Sci Rep. 2016 Nov 10;6:36485. doi: 10.1038/srep36485.

15.

Rational Design, Synthesis and Evaluation of Coumarin Derivatives as Protein-protein Interaction Inhibitors.

De Luca L, Agharbaoui FE, Gitto R, Buemi MR, Christ F, Debyser Z, Ferro S.

Mol Inform. 2016 Sep;35(8-9):460-73. doi: 10.1002/minf.201501034. Epub 2016 Jul 25.

PMID:
27546050
16.

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;8:248-264. doi: 10.1016/j.ebiom.2016.04.039. Epub 2016 May 13.

17.

Lessons Learned: HIV Points the Way Towards Precision Treatment of Mixed-Lineage Leukemia.

Cermakova K, Weydert C, Christ F, De Rijck J, Debyser Z.

Trends Pharmacol Sci. 2016 Aug;37(8):660-671. doi: 10.1016/j.tips.2016.05.005. Epub 2016 Jun 9. Review.

PMID:
27290878
18.

2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4.

Billamboz M, Suchaud V, Bailly F, Lion C, Andréola ML, Christ F, Debyser Z, Cotelle P.

Eur J Med Chem. 2016 Jul 19;117:256-68. doi: 10.1016/j.ejmech.2016.03.083. Epub 2016 Mar 28.

PMID:
27105029
19.

HIV-1 integrase inhibition: looking at cofactor interactions.

Christ F, Debyser Z.

Future Med Chem. 2015;7(18):2407-10. doi: 10.4155/fmc.15.162. Epub 2015 Dec 15. No abstract available.

20.

Kuwanon-L as a New Allosteric HIV-1 Integrase Inhibitor: Molecular Modeling and Biological Evaluation.

Esposito F, Tintori C, Martini R, Christ F, Debyser Z, Ferrarese R, Cabiddu G, Corona A, Ceresola ER, Calcaterra A, Iovine V, Botta B, Clementi M, Canducci F, Botta M, Tramontano E.

Chembiochem. 2015 Nov;16(17):2507-12. doi: 10.1002/cbic.201500385. Epub 2015 Oct 26.

PMID:
26360521
21.

Targeting Virus-host Interactions of HIV Replication.

Weydert C, De Rijck J, Christ F, Debyser Z.

Curr Top Med Chem. 2016;16(10):1167-90. Review.

PMID:
26324041
22.

Multiple cellular proteins interact with LEDGF/p75 through a conserved unstructured consensus motif.

Tesina P, Čermáková K, Hořejší M, Procházková K, Fábry M, Sharma S, Christ F, Demeulemeester J, Debyser Z, Rijck J, Veverka V, Řezáčová P.

Nat Commun. 2015 Aug 6;6:7968. doi: 10.1038/ncomms8968.

PMID:
26245978
23.

Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75.

Cuzzucoli Crucitti G, Pescatori L, Messore A, Madia VN, Pupo G, Saccoliti F, Scipione L, Tortorella S, Di Leva FS, Cosconati S, Novellino E, Debyser Z, Christ F, Costi R, Di Santo R.

Eur J Med Chem. 2015 Aug 28;101:288-94. doi: 10.1016/j.ejmech.2015.06.036. Epub 2015 Jun 22.

PMID:
26150289
24.

Optimization of rhodanine scaffold for the development of protein-protein interaction inhibitors.

Ferro S, De Luca L, Agharbaoui FE, Christ F, Debyser Z, Gitto R.

Bioorg Med Chem. 2015 Jul 1;23(13):3208-14. doi: 10.1016/j.bmc.2015.04.072. Epub 2015 May 2.

PMID:
25999203
25.

HIV-1 IN/Pol recruits LEDGF/p75 into viral particles.

Desimmie BA, Weydert C, Schrijvers R, Vets S, Demeulemeester J, Proost P, Paron I, De Rijck J, Mast J, Bannert N, Gijsbers R, Christ F, Debyser Z.

Retrovirology. 2015 Feb 12;12:16. doi: 10.1186/s12977-014-0134-4.

26.

Host factors for retroviral integration site selection.

Debyser Z, Christ F, De Rijck J, Gijsbers R.

Trends Biochem Sci. 2015 Feb;40(2):108-16. doi: 10.1016/j.tibs.2014.12.001. Epub 2014 Dec 31. Review.

PMID:
25555456
27.

Nogo-A deletion increases the plasticity of the optokinetic response and changes retinal projection organization in the adult mouse visual system.

Guzik-Kornacka A, van der Bourg A, Vajda F, Joly S, Christ F, Schwab ME, Pernet V.

Brain Struct Funct. 2016 Jan;221(1):317-29. doi: 10.1007/s00429-014-0909-3. Epub 2014 Oct 5.

PMID:
25284126
28.

Cell type-specific Nogo-A gene ablation promotes axonal regeneration in the injured adult optic nerve.

Vajda F, Jordi N, Dalkara D, Joly S, Christ F, Tews B, Schwab ME, Pernet V.

Cell Death Differ. 2015 Feb;22(2):323-35. doi: 10.1038/cdd.2014.147. Epub 2014 Sep 26.

29.

Design and discovery of 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide inhibitors of HIV-1 integrase.

Zhang D, Debnath B, Yu S, Sanchez TW, Christ F, Liu Y, Debyser Z, Neamati N, Zhao G.

Bioorg Med Chem. 2014 Oct 1;22(19):5446-53. doi: 10.1016/j.bmc.2014.07.036. Epub 2014 Jul 30.

PMID:
25150089
30.

The HIV-1 integrase mutant R263A/K264A is 2-fold defective for TRN-SR2 binding and viral nuclear import.

De Houwer S, Demeulemeester J, Thys W, Rocha S, Dirix L, Gijsbers R, Christ F, Debyser Z.

J Biol Chem. 2014 Sep 5;289(36):25351-61. doi: 10.1074/jbc.M113.533281. Epub 2014 Jul 25.

31.

Structure of transportin SR2, a karyopherin involved in human disease, in complex with Ran.

Tsirkone VG, Beutels KG, Demeulemeester J, Debyser Z, Christ F, Strelkov SV.

Acta Crystallogr F Struct Biol Commun. 2014 Jun;70(Pt 6):723-9. doi: 10.1107/S2053230X14009492. Epub 2014 May 24.

32.

4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors.

Billamboz M, Suchaud V, Bailly F, Lion C, Demeulemeester J, Calmels C, Andréola ML, Christ F, Debyser Z, Cotelle P.

ACS Med Chem Lett. 2013 May 17;4(7):606-11. doi: 10.1021/ml400009t. eCollection 2013 Jul 11.

33.

Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors.

Suchaud V, Bailly F, Lion C, Calmels C, Andréola ML, Christ F, Debyser Z, Cotelle P.

J Med Chem. 2014 Jun 12;57(11):4640-60. doi: 10.1021/jm500109z. Epub 2014 May 14.

PMID:
24793360
34.

Diketoacid chelating ligands as dual inhibitors of HIV-1 integration process.

Rogolino D, Carcelli M, Compari C, De Luca L, Ferro S, Fisicaro E, Rispoli G, Neamati N, Debyser Z, Christ F, Chimirri A.

Eur J Med Chem. 2014 May 6;78:425-30. doi: 10.1016/j.ejmech.2014.03.070. Epub 2014 Mar 25.

PMID:
24704615
35.

LEDGINs, non-catalytic site inhibitors of HIV-1 integrase: a patent review (2006 - 2014).

Demeulemeester J, Chaltin P, Marchand A, De Maeyer M, Debyser Z, Christ F.

Expert Opin Ther Pat. 2014 Jun;24(6):609-32. doi: 10.1517/13543776.2014.898753. Epub 2014 Mar 25. Review.

PMID:
24666332
36.

A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition.

Ferro S, De Luca L, Lo Surdo G, Morreale F, Christ F, Debyser Z, Gitto R, Chimirri A.

Bioorg Med Chem. 2014 Apr 1;22(7):2269-79. doi: 10.1016/j.bmc.2014.02.012. Epub 2014 Feb 20.

PMID:
24618511
37.

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
38.

Identification of small peptides inhibiting the integrase-LEDGF/p75 interaction through targeting the cellular co-factor.

Cavalluzzo C, Christ F, Voet A, Sharma A, Singh BK, Zhang KY, Lescrinier E, De Maeyer M, Debyser Z, Van der Eycken E.

J Pept Sci. 2013 Oct;19(10):651-8. doi: 10.1002/psc.2543. Epub 2013 Aug 27.

PMID:
24014475
39.

New scaffolds of natural origin as Integrase-LEDGF/p75 interaction inhibitors: virtual screening and activity assays.

De Luca L, Morreale F, Christ F, Debyser Z, Ferro S, Gitto R.

Eur J Med Chem. 2013 Oct;68:405-11. doi: 10.1016/j.ejmech.2013.07.025. Epub 2013 Aug 9.

PMID:
23994868
40.

Discovery of a novel 5-carbonyl-1H-imidazole-4-carboxamide class of inhibitors of the HIV-1 integrase-LEDGF/p75 interaction.

Serrao E, Xu ZL, Debnath B, Christ F, Debyser Z, Long YQ, Neamati N.

Bioorg Med Chem. 2013 Oct 1;21(19):5963-72. doi: 10.1016/j.bmc.2013.07.047. Epub 2013 Aug 2.

41.

Interaction of transportin-SR2 with Ras-related nuclear protein (Ran) GTPase.

Taltynov O, Demeulemeester J, Christ F, De Houwer S, Tsirkone VG, Gerard M, Weeks SD, Strelkov SV, Debyser Z.

J Biol Chem. 2013 Aug 30;288(35):25603-13. doi: 10.1074/jbc.M113.484345. Epub 2013 Jul 22.

42.

Synthesis and biological evaluation of novel antiviral agents as protein-protein interaction inhibitors.

Ferro S, De Luca L, Morreale F, Christ F, Debyser Z, Gitto R, Chimirri A.

J Enzyme Inhib Med Chem. 2014 Apr;29(2):237-42. doi: 10.3109/14756366.2013.766609. Epub 2013 Jul 16.

PMID:
23859152
43.

Design of cell-permeable stapled peptides as HIV-1 integrase inhibitors.

Long YQ, Huang SX, Zawahir Z, Xu ZL, Li H, Sanchez TW, Zhi Y, De Houwer S, Christ F, Debyser Z, Neamati N.

J Med Chem. 2013 Jul 11;56(13):5601-12. doi: 10.1021/jm4006516. Epub 2013 Jun 24.

44.

LEDGINs inhibit late stage HIV-1 replication by modulating integrase multimerization in the virions.

Desimmie BA, Schrijvers R, Demeulemeester J, Borrenberghs D, Weydert C, Thys W, Vets S, Van Remoortel B, Hofkens J, De Rijck J, Hendrix J, Bannert N, Gijsbers R, Christ F, Debyser Z.

Retrovirology. 2013 May 30;10:57. doi: 10.1186/1742-4690-10-57.

45.

2-Hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs), novel inhibitors of HIV integrase with a high barrier to resistance.

Desimmie BA, Demeulemeester J, Suchaud V, Taltynov O, Billamboz M, Lion C, Bailly F, Strelkov SV, Debyser Z, Cotelle P, Christ F.

ACS Chem Biol. 2013;8(6):1187-94. doi: 10.1021/cb4000426. Epub 2013 Apr 2.

PMID:
23517458
46.

Single-cell imaging of HIV-1 provirus (SCIP).

Di Primio C, Quercioli V, Allouch A, Gijsbers R, Christ F, Debyser Z, Arosio D, Cereseto A.

Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5636-41. doi: 10.1073/pnas.1216254110. Epub 2013 Mar 19.

47.

Fragment-based discovery of 8-hydroxyquinoline inhibitors of the HIV-1 integrase-lens epithelium-derived growth factor/p75 (IN-LEDGF/p75) interaction.

Serrao E, Debnath B, Otake H, Kuang Y, Christ F, Debyser Z, Neamati N.

J Med Chem. 2013 Mar 28;56(6):2311-22. doi: 10.1021/jm301632e. Epub 2013 Mar 18.

48.

Impairing MLL-fusion gene-mediated transformation by dissecting critical interactions with the lens epithelium-derived growth factor (LEDGF/p75).

Méreau H, De Rijck J, Cermáková K, Kutz A, Juge S, Demeulemeester J, Gijsbers R, Christ F, Debyser Z, Schwaller J.

Leukemia. 2013 Jun;27(6):1245-53. doi: 10.1038/leu.2013.10. Epub 2013 Jan 15.

PMID:
23318960
49.

Discovery of novel inhibitors of LEDGF/p75-IN protein-protein interactions.

Sanchez TW, Debnath B, Christ F, Otake H, Debyser Z, Neamati N.

Bioorg Med Chem. 2013 Feb 15;21(4):957-63. doi: 10.1016/j.bmc.2012.12.012. Epub 2012 Dec 20.

50.

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.

Supplemental Content

Loading ...
Support Center