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Items: 1 to 20 of 115

1.

Small molecule inhibitors of the LEDGF site of human immunodeficiency virus integrase identified by fragment screening and structure based design.

Peat TS, Rhodes DI, Vandegraaff N, Le G, Smith JA, Clark LJ, Jones ED, Coates JA, Thienthong N, Newman J, Dolezal O, Mulder R, Ryan JH, Savage GP, Francis CL, Deadman JJ.

PLoS One. 2012;7(7):e40147. doi: 10.1371/journal.pone.0040147. Epub 2012 Jul 10. Erratum in: PLoS One. 2013;8(7). doi:10.1371/annotation/eb238f0f-7582-4318-af95-64ac98d3b0be.

2.

Crystal structures of novel allosteric peptide inhibitors of HIV integrase identify new interactions at the LEDGF binding site.

Rhodes DI, Peat TS, Vandegraaff N, Jeevarajah D, Newman J, Martyn J, Coates JA, Ede NJ, Rea P, Deadman JJ.

Chembiochem. 2011 Oct 17;12(15):2311-5. doi: 10.1002/cbic.201100350. Epub 2011 Aug 17.

PMID:
21850718
3.

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
4.
5.

Screening for antiviral inhibitors of the HIV integrase-LEDGF/p75 interaction using the AlphaScreen luminescent proximity assay.

Hou Y, McGuinness DE, Prongay AJ, Feld B, Ingravallo P, Ogert RA, Lunn CA, Howe JA.

J Biomol Screen. 2008 Jun;13(5):406-14. doi: 10.1177/1087057108317060. Epub 2008 May 14.

PMID:
18480474
6.

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
7.

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
8.

Fragment hopping approach directed at design of HIV IN-LEDGF/p75 interaction inhibitors.

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

J Enzyme Inhib Med Chem. 2013 Oct;28(5):1002-9. doi: 10.3109/14756366.2012.703184. Epub 2012 Jul 18.

PMID:
22803661
9.

A New Class of Allosteric HIV-1 Integrase Inhibitors Identified by Crystallographic Fragment Screening of the Catalytic Core Domain.

Patel D, Antwi J, Koneru PC, Serrao E, Forli S, Kessl JJ, Feng L, Deng N, Levy RM, Fuchs JR, Olson AJ, Engelman AN, Bauman JD, Kvaratskhelia M, Arnold E.

J Biol Chem. 2016 Nov 4;291(45):23569-23577. Epub 2016 Sep 19.

PMID:
27645997
10.

Affinities between the binding partners of the HIV-1 integrase dimer-lens epithelium-derived growth factor (IN dimer-LEDGF) complex.

Tsiang M, Jones GS, Hung M, Mukund S, Han B, Liu X, Babaoglu K, Lansdon E, Chen X, Todd J, Cai T, Pagratis N, Sakowicz R, Geleziunas R.

J Biol Chem. 2009 Nov 27;284(48):33580-99. doi: 10.1074/jbc.M109.040121. Epub 2009 Sep 28.

11.

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.

12.

Differential interaction of HIV-1 integrase and JPO2 with the C terminus of LEDGF/p75.

Bartholomeeusen K, De Rijck J, Busschots K, Desender L, Gijsbers R, Emiliani S, Benarous R, Debyser Z, Christ F.

J Mol Biol. 2007 Sep 14;372(2):407-21. Epub 2007 Jul 12.

PMID:
17669426
13.

Insights into the interactions between HIV-1 integrase and human LEDGF/p75 by molecular dynamics simulation and free energy calculation.

Zhao Y, Li W, Zeng J, Liu G, Tang Y.

Proteins. 2008 Aug;72(2):635-45. doi: 10.1002/prot.21955.

PMID:
18247352
14.

Pharmacophore-based discovery of small-molecule inhibitors of protein-protein interactions between HIV-1 integrase and cellular cofactor LEDGF/p75.

De Luca L, Barreca ML, Ferro S, Christ F, Iraci N, Gitto R, Monforte AM, Debyser Z, Chimirri A.

ChemMedChem. 2009 Aug;4(8):1311-6. doi: 10.1002/cmdc.200900070.

PMID:
19565598
15.

1,4-Bis(5-(naphthalen-1-yl)thiophen-2-yl)naphthalene, a small molecule, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular Lens epithelium-derived growth factor.

Gu WG, Ip DT, Liu SJ, Chan JH, Wang Y, Zhang X, Zheng YT, Wan DC.

Chem Biol Interact. 2014 Apr 25;213:21-7. doi: 10.1016/j.cbi.2014.01.011. Epub 2014 Jan 28.

PMID:
24480521
16.

Structural properties of HIV integrase. Lens epithelium-derived growth factor oligomers.

Gupta K, Diamond T, Hwang Y, Bushman F, Van Duyne GD.

J Biol Chem. 2010 Jun 25;285(26):20303-15. doi: 10.1074/jbc.M110.114413. Epub 2010 Apr 20.

17.

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.

18.
19.

Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor.

De Luca L, Ferro S, Gitto R, Barreca ML, Agnello S, Christ F, Debyser Z, Chimirri A.

Bioorg Med Chem. 2010 Nov 1;18(21):7515-21. doi: 10.1016/j.bmc.2010.08.051. Epub 2010 Sep 17.

PMID:
20850978
20.

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.

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