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HIV smallPublications in International Scientific Journals

2011

  • Gijsbers R, Vets S, De Rijck J, Ocwieja K, Ronen K, Malani N, Bushman FD, Debyser Z. Role Of The PWWP Domain Of LEDGF/P75 In Lentiviral Integration Targeting. J Biol Chem. 2011 Oct 10. [Epub ahead of print] [Pubmed] [pdf]

  • Ferro S, Grazia SD, De Luca L, Gitto R, Faliti CE, Debyzer Z, Chimirri A. Microwave Assisted Organic Synthesis (MAOS) of Small Molecules as Potential HIV-1 Integrase Inhibitors. Molecules16(8): 6858-6870. [Pubmed] [pdf]

  • Schrijvers R, Desimmie BA, Debyser Z. Rilpivirine: a step forward in tailored HIV treatment. Lancet. 2011 Jul 16;378(9787):201-3. [Pubmed] [pdf]

  • McNeely M, Hendrix J, Busschots K, Boons E, Deleersnijder A, Gerard M, Christ F, Debyser Z. In Vitro DNA Tethering of HIV-1 Integrase by the Transcriptional Coactivator LEDGF/p75. J Mol Biol. 410(5):811-30. [Pubmed] [pdf]

  • Allouch A, Di Primio C, Alpi E, Lusic M, Arosio D, Giacca M, Cereseto A. The TRIM family protein KAP1 inhibits HIV-1 integration. Cell Host Microbe. 2011 Jun 16;9(6):484-95. [Pubmed] [no pdf]

  • Francis AC, Di Primio C, Allouch A, Cereseto A. Role of Phosphorylation in the Nuclear Biology of HIV-1. Curr Med Chem. 2011;18(19):2904-12. [Pubmed] [no pdf]

  • De Luca L, Gitto R, Christ F, Ferro S, De Grazia S, Morreale F, Debyser Z, Chimirri A. 4-[1-(4-Fluorobenzyl)-4-hydroxy-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acid as a prototype to develop dual inhibitors of HIV-1 integration process. Antiviral Res 92(1):102-7. [Pubmed] [pdf]

  • Madlala P, Gijsbers R, Christ F, Hombrouck A, Werner L, Mlisana K, An P, Karim SS, Winkler CA, Debyser Z, Ndungʼu T. Association of Polymorphisms in the LEDGF/p75 Gene (PSIP1) with Susceptibility to HIV-1 Infection and Disease Progression. AIDS 25(14):1711-9. [Pubmed] [pdf].

  • Rinaldi M, Tintori C, Franchi L, Vignaroli G, Innitzer A, Massa S, Esté JA, Gonzalo E, Christ F, Debyser Z, Botta M. A Versatile and Practical Synthesis toward the Development of Novel HIV-1 Integrase Inhibitors. ChemMedChem. 2011 Jan 18. doi: 10.1002/cmdc.201000510. [Epub ahead of print] [Pubmed] [pdf]

  • De Luca L, Ferro S, Morreale F, Chimirri A. Inhibition of the Interaction between HIV-1 Integrase and its Cofactor LEDGF/p75: A Promising Approach in Anti-Retroviral Therapy. Mini Rev Med Chem. 11(8):714-27. [Pubmed] [pdf]

  • De Luca L, Ferro S, Morreale F, De Grazia S, Chimirri A. Inhibitors of the Interactions between HIV-1 IN and the Cofactor LEDGF/p75. ChemMedChem. 6(7):1184-91. [Pubmed] [pdf]

  • De Luca L, De Grazia S, Ferro S, Gitto R, Christ F, Debyser Z, Chimirri A. HIV-1 integrase strand-transfer inhibitors: Design, synthesis and molecular modeling investigation. Eur J Med Chem. 46 (2): 756-764. [Pubmed] [pdf]

  • Hendrix J, Gijsbers R, De Rijck J, Voet A, Hotta J-i, McNeely M, Hofkens J, Debyser Z, Engelborghs Y. The transcriptional co-activator LEDGF/p75 displays a dynamic scan-and-lock mechanism for chromatin tethering. Nucleic Acid Research 39(4):1310-1325. [Pubmed] [pdf]

  • Thys W, De Houwer S, Demeulemeester J, Taltynov O, Vancraenenbroeck R, Gérard M, De Rijck J, Gijsbers R, Christ F, Debyser Z. Interplay between HIV entry and transportin-SR2 dependency. Retrovirology 8(1):7. [Pubmed] [pdf]

2010

  • De Luca L, Ferro S, Gitto R, Barreca ML, Agnello S, Christ F, Debyser Z, Chimirri A. Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor. Bioorg Med Chem. 18(21):7515-21. [Pubmed] [pdf]

  • Terreni M, Valentini P, Liverani V, Gutierrez MI, Di Primio C, Di Fenza A, Tozzini V, Allouch A, Albanese A, Giacca M, Cereseto A. GCN5-dependent acetylation of HIV-1 integrase enhances viral integration. Retrovirology 7:18. [Pubmed] [pdf]

  • Ferro S, De Luca L, Barreca ML, De Grazia S, Christ F, Debyser Z, Chimirri Alba. New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action. Bioorg med chem 18(15):5510-8. [Pubmed] [pdf]

  • 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. Rational design of first-in-class inhibitors of LEDGF/p75-integrase interaction and HIV replication. Nature Chemical Biology 6(6):442-8. [Pubmed link] [pdf] [supplement]

  • De Rijck J, Bartholomeeusen K, Ceulemans H, Debyser Z, Gijsbers R. High-resolution profiling of the LEDGF/p75 chromatin interaction in the ENCODE region. Nucleic Acids Research 38(18):6135-47. [Pubmed link] [pdf].

  • Gijsbers R, Ronen K, Vets S, Malani N, De Rijck J, McNeely M, Bushman F, Debyser Z. LEDGF hybrids efficiently retarget lentiviral integration into heterochromatin. Molecular Therapy 18(3): 552-560. [Pubmed link] [pdf]

2009

  • Barreca ML, Iraci N, De Luca L, Chimirri A. Induced-Fit Docking Approach Provides Insight into the Binding Mode and Mechanism of Action of HIV-1 Integrase Inhibitors. Chem Med Chem 4(9):1446-56. [Pubmed link] [pdf]

  • Bartholomeeusen K, Gijsbers R, Christ F, Hendrix J, Rain JC, Emiliani S, Benarous R, Debyser Z, De Rijck J. Lens Epithelium Derived Growth Factor/p75 interacts with the transposase derived DDE domain of pogZ. J Biol Chem. 284(17):11467-77.[Pubmed link] [pdf]

  • De Luca L, Barreca ML, Ferro S, Christ F, Iraci N, Gitto R, Monforte AM, Debyser Z, Chimirri A. Pharmacophore-Based Discovery of Small-Molecule Inhibitors of Protein-Protein Interactions between HIV-1 Integrase and Cellular Cofactor LEDGF/p75 ChemMedChem. 4(8):1311-6. [Pubmed link] [pdf]

  • Ferro S, Agnello S, Barreca ML, De Luca L, Christ F, Gitto R. Synthesis of New Pyridazine Derivatives as Potential Anti-HIV-1 Agents. J Heterocyclic Chem 46(6): 1420-1424.[Web of Science link] [pdf]

  • Ferro S, De Grazia S, De Luca L, Barreca ML, Debyser Z, Chimirri A. Structural modification of diketo acid portion in 1h-benzylindole derivatives hiv-1 integrase inhibitors. Heterocycles 78(4): 947-959. [Web of Science link] [pdf]

  • Ferro S, De Luca L, Barreca ML, Iraci N, De Grazia S, Christ F, Witvrouw M, Debyser Z, Chimirri A. Docking studies on a new human immunodeficiency virus integrase-Mg-DNA complex: phenyl ring exploration and synthesis of 1H-benzylindole derivatives through fluorine substitutions. J Med Chem. 52(2):569-73. [Pubmed link] [pdf]

  • Rajamaki S, Innitzer A, Falciani C, Tintori C, Christ F, Witvrouw M, Debyser Z, Massa S, Botta M. Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors. Bioorg Med Chem Lett. 19(13):3615-8. [Pubmed link] [pdf]

  • Thys W, Busschots K, McNeely M, Voet A, Christ F, Debyser Z. LEDGF/p75 and transportin-SR2 are cellular cofactors of HIV integrase and novel targets for antiviral therapy. HIV Ther. 2009, 3(2), 171–188. [no Pubmed link] [pdf]

  • Voet ARD, De Maeyer M, Debyser Z, Christ F. In search of second-generation HIV integrase inhibitors: targeting integration beyond strand transfer. Future Med Chem 1(7):1259-1274. [Abstract] [No Pubmed link] [pdf]

 

2008

  • Albanese A, Arosio D, Terreni M, Cereseto A. HIV-1 pre-integration complexes selectively target decondensed chromatin in the nuclear periphery. PLoS ONE 3 (6):e2413. [Free Access]

  • Christ F, Thys W, De Rijck J, Gijsbers R, Albanese A, Arosio D, Emiliani S, Rain JC, Benarous R, Cereseto A, Debyser Z. Transportin-SR2 imports HIV into the nucleus. Curr Biol. 18(16):1192-202. [Pubmed link] [pdf] [Supplements]

  • Billamboz M, Bailly F, Barreca ML, De Luca L, Mouscadet JF, Calmels C, Andréola ML, Witvrouw M, Christ F, Debyser Z, Cotelle P. Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain. J Med Chem. 51(24):7717-30. [Pubmed link] [pdf]

  • Hombrouck A, Van Remoortel B, Michiels M, Noppe W, Christ F, Eneroth A, Sahlberg BL, Benkestock K, Vrang L, Johansson NG, Barreca ML, De Luca L, Ferro S, Chimirri A, Debyser Z, Witvrouw M. Preclinical Evaluation of 1H-Benzylindole Derivatives as Novel Human Immunodeficiency Virus Integrase Stran Transfer Inhibitors. Antimicrob Agents Chemother 2008 52(8)2861-1869. [Pubmed link] [pdf]

  • De Luca L, Barreca ML, Ferro S, Iraci N, Michiels M, Christ F, Debyser Z, Witvrouw M, Chimirri A. A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series. Bioorg Med Chem Lett. 18(9):2891-5. [Pubmed link] [pdf]