Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium, Annals of the New York Academy of Sciences, vol.50, issue.1, pp.83-89, 2011. ,
DOI : 10.1111/j.1749-6632.2011.05972.x
Retroviral intasome assembly and inhibition of DNA strand transfer, Nature, vol.25, issue.7286, pp.232-236, 2010. ,
DOI : 10.1038/nature08784
Resistance to HIV-1 integrase inhibitors: A structural perspective, Drug Resistance Updates, vol.13, issue.4-5, pp.139-150, 2010. ,
DOI : 10.1016/j.drup.2010.05.001
Evolution of HIV integrase resistance mutations, Current Opinion in Infectious Diseases, vol.26, pp.43-49, 2013. ,
DOI : 10.1097/QCO.0b013e32835ba81c
Structural and Functional Analyses of the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir (S/GSK1349572), Molecular Pharmacology, vol.80, issue.4 ,
DOI : 10.1124/mol.111.073189
Viral fitness cost prevents HIV-1 from evading dolutegravir drug pressure, Retrovirology, vol.10, issue.1, p.22, 2013. ,
DOI : 10.1038/nature08784
HIV-1 Integrase Forms Stable Tetramers and Associates with LEDGF/p75 Protein in Human Cells, Journal of Biological Chemistry, vol.278, issue.1, pp.372-381, 2003. ,
DOI : 10.1074/jbc.M209278200
Proteinprotein interactions in human immunodeficiency virus International publication number WO 03, 333346P Nov, vol.26, 2001. ,
The Lentiviral Integrase Binding Protein LEDGF/p75 and HIV-1 Replication, PLoS Pathogens, vol.4, issue.3, p.1000046, 2008. ,
DOI : 10.1371/journal.ppat.1000046.g004
The Interaction of LEDGF/p75 with Integrase Is Lentivirus-specific and Promotes DNA Binding, Journal of Biological Chemistry, vol.280, issue.18, pp.17841-17847, 2005. ,
DOI : 10.1074/jbc.M411681200
Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75, Proceedings of the National Academy of Sciences, vol.102, issue.48, pp.17308-17313, 2005. ,
DOI : 10.1073/pnas.0506924102
A Novel Co-Crystal Structure Affords the Design of Gain-of-Function Lentiviral Integrase Mutants in the Presence of Modified PSIP1/LEDGF/p75, PLoS Pathogens, vol.81, issue.1, p.1000259, 2009. ,
DOI : 10.1371/journal.ppat.1000259.s005
An Essential Role for LEDGF/p75 in HIV Integration, Science, vol.314, issue.5798, pp.461-464, 2006. ,
DOI : 10.1126/science.1132319
LEDGF/p75 functions downstream from preintegration complex formation to effect gene-specific HIV-1 integration, Genes & Development, vol.21, issue.14, pp.1767-1778, 2007. ,
DOI : 10.1101/gad.1565107
A role for LEDGF/p75 in targeting HIV DNA integration, Nature Medicine, vol.17, issue.12, pp.1287-1289, 2005. ,
DOI : 10.1038/nm1329
Structural Basis for Functional Tetramerization of Lentiviral Integrase, PLoS Pathogens, vol.331, issue.7, p.1000515, 2009. ,
DOI : 10.1371/journal.ppat.1000515.s007
Integrase Mutants Defective for Interaction with LEDGF/p75 Are Impaired in Chromosome Tethering and HIV-1 Replication, Journal of Biological Chemistry, vol.280, issue.27, pp.25517-25523, 2005. ,
DOI : 10.1074/jbc.M501378200
Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication, Nature Chemical Biology, vol.70, issue.6, pp.442-448, 2010. ,
DOI : 10.1038/nchembio.370
Preparation of pyrazolylbenzimidazole derivatives for use as HIV replication inhibitors, Boehringer Ingelheim International GmbH, pp.67644-67645, 2008. ,
Preparation of 2-(tert-butyloxy)- 2-(2-methylquinolin-3-yl)acetic acid derivatives as inhibitors of human immunodeficiency virus replication, Boehringer Ingelheim International GmbH, pp.62285-62286, 2009. ,
Preparation of 2-alkoxy-2-(pyridin-3-yl)acetic acid derivatives as inhibitors of human immunodeficiency virus (HIV) replication. Boehringer Ingelheim International GmbH, pp.130034-130035, 2010. ,
Identification of BI-C, a Novel HIV-1 non- Catalytic Site Integrase Inhibitor, p.18, 2011. ,
Benzothiazole Compounds and Their Pharmaceutical use. US: Gilead Sciences Inc, pp.145728-145729, 2012. ,
Pyrimidine Derivatives as Novel Viral Replication Inhibitors and Their Preparation and use in the Treatment of HIV Infection ,
Naphth-2-yl)Acetic Acid Derivatives as HIV Antiviral Agents and Their Preparation and use for the Treatment of AIDS, pp.2-003497, 2012. ,
-(Quinolin-6-yl)Acetic Acid Derivatives as HIV Antiviral Agents and Their Preparation and use for the Treatment of AIDS. USA: Gilead Sciences, Inc, p.144 ,
Inhibitors of HIV Replication ,
Inhibitors of Human Immunodeficiency Virus Replication. US: Bristol Myers Squibb Co ,
Isoquinoline Compounds and Methods for Treating HIV. US: Glaxo Smithkline LLC, pp.102985-102986, 2012. ,
Inhibitors of Viral Replication, Their Process of Preparation and Their Therapeutical Uses, Laboratoire Biodim, FR, pp.137181-137182, 2012. ,
Inhibitors of viral replication, their process of preparation and their therapeutical uses. Laboratoire Biodim FR 2012, pp.140243-140244 ,
Small-Molecule Inhibitors of the LEDGF/p75 Binding Site of Integrase Block HIV Replication and Modulate Integrase Multimerization, Antimicrobial Agents and Chemotherapy, vol.56, issue.8, pp.4365-4374, 2012. ,
DOI : 10.1128/AAC.00717-12
New Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action, Journal of Biological Chemistry, vol.287, issue.25, pp.21189-21203, 2012. ,
DOI : 10.1074/jbc.M112.347534
Multimode, Cooperative Mechanism of Action of Allosteric HIV-1 Integrase Inhibitors, Journal of Biological Chemistry, vol.287, issue.20, pp.16801-16811, 2012. ,
DOI : 10.1074/jbc.M112.354373
Development of an AlphaScreen-Based HIV-1 Integrase Dimerization Assay for Discovery of Novel Allosteric Inhibitors, Journal of Biomolecular Screening, vol.582, issue.5, pp.618-628, 2012. ,
DOI : 10.1021/jm901137j
The LEDGF/p75 integrase interaction, a novel target for anti-HIV therapy, Virology, vol.435, issue.1, pp.102-109, 2013. ,
DOI : 10.1016/j.virol.2012.09.033
HRP2 determines the efficiency and specificity of HIV-1 integration in LEDGF/p75 knockout cells but does not contribute to the antiviral activity of a potent LEDGF/p75-binding site integrase inhibitor, Nucleic Acids Research, vol.40, issue.22, pp.11518-11530, 2012. ,
DOI : 10.1093/nar/gks913
The A128T Resistance Mutation Reveals Aberrant Protein Multimerization as the Primary Mechanism of Action of Allosteric HIV-1 Integrase Inhibitors, Journal of Biological Chemistry, vol.288, issue.22, pp.15813-15820, 2013. ,
DOI : 10.1074/jbc.M112.443390
LEDGINs inhibit late stage HIV-1 replication by modulating integrase multimerization in the virions, Retrovirology, vol.10, issue.1, p.57, 2013. ,
DOI : 10.1016/j.ab.2005.05.015
Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation, Proceedings of the National Academy of Sciences, vol.110, issue.21, pp.8690-8695, 2013. ,
DOI : 10.1073/pnas.1300703110
Non-Catalytic Site Integrase Inhibitors Target the Integrase Domain During Virus Production and Induce a Reverse Transcription Block, Conference on Retroviruses and Opportunistic Infections. Gilead Sciences, 2013. ,
Non-Catalytic Site HIV-1 Integrase Inhibitors Disrupt Core Maturation and Induce a Reverse Transcription Block in Target Cells, PLoS ONE, vol.8, issue.9, p.74163, 2013. ,
DOI : 10.1371/journal.pone.0074163.s002
Inhibiting HIV-1 integrase by shifting its oligomerization equilibrium, Proceedings of the National Academy of Sciences, vol.104, issue.20, pp.8316-8321, 2007. ,
DOI : 10.1073/pnas.0700781104
Resistance Studies with HIV-1 non-Catalytic Site Integrase Inhibitors, International Workshop on HIV & Hepatitis Virus Drug Resistance and Curative Strategies, 2011. ,
HeLa-LAV, an epithelial cell line stably infected with HIV-1, Journal of Virological Methods, vol.34, issue.2, pp.173-180, 1991. ,
DOI : 10.1016/0166-0934(91)90097-J
Relationship between the Oligomeric Status of HIV-1 Integrase on DNA and Enzymatic Activity, Journal of Biological Chemistry, vol.281, issue.32, pp.22707-22719, 2006. ,
DOI : 10.1074/jbc.M602198200
URL : https://hal.archives-ouvertes.fr/hal-00216092
The Pleiotropic Nature of Human Immunodeficiency Virus Type 1 Integrase Mutations. In HIV-1 Integrase: Mechanism and Inhibitor Design, Drug Discovery and Development, pp.67-81 ,
Structure of a two-domain fragment of HIV-1 integrase: implications for domain organization in the intact protein, The EMBO Journal, vol.20, issue.24, pp.7333-7343, 2001. ,
DOI : 10.1093/emboj/20.24.7333
The role of lysine 186 in HIV-1 integrase multimerization, Virology, vol.364, issue.1, pp.227-236, 2007. ,
DOI : 10.1016/j.virol.2007.02.029
In vitro initial attachment of HIV-1 integrase to viral ends: control of the DNA specific interaction by the oligomerization state, Nucleic Acids Research, vol.36, issue.22, pp.7043-7058, 2008. ,
DOI : 10.1093/nar/gkn796
URL : https://hal.archives-ouvertes.fr/hal-00426343
Interfacial inhibitors: targeting macromolecular complexes, Nat Rev Drug Discov, vol.11, pp.25-36, 2012. ,
In vivo emergence of HIV-1 variants resistant to multiple
protease inhibitors, Nature, vol.374, issue.6522, pp.569-571, 1995. ,
DOI : 10.1038/374569a0
Colinearity of Reverse Transcriptase Inhibitor Resistance Mutations Detected by Population-Based Sequencing, JAIDS Journal of Acquired Immune Deficiency Syndromes, vol.34, issue.4, pp.398-402, 2003. ,
DOI : 10.1097/00126334-200312010-00006
The G140S mutation in HIV integrases from raltegravir-resistant patients rescues catalytic defect due to the resistance Q148H mutation, Nucleic Acids Research, vol.37, issue.4, pp.1193-1201, 2009. ,
DOI : 10.1093/nar/gkn1050
Analysis of Early Human Immunodeficiency Virus Type 1 DNA Synthesis by Use of a New Sensitive Assay for Quantifying Integrated Provirus, Journal of Virology, vol.77, issue.18, pp.10119-10124, 2003. ,
DOI : 10.1128/JVI.77.18.10119-10124.2003
Structural basis for HIV-1 DNA integration in the human genome, role of the LEDGF/P75 cofactor, The EMBO Journal, vol.269, issue.7, pp.980-991, 2009. ,
DOI : 10.1073/pnas.93.24.13659
URL : https://hal.archives-ouvertes.fr/inserm-00384501
Domains of the integrase protein of human immunodeficiency virus type 1 responsible for polynucleotidyl transfer and zinc binding., Proceedings of the National Academy of Sciences, vol.90, issue.8, pp.3428-3432, 1993. ,
DOI : 10.1073/pnas.90.8.3428
Catalytic domain of human immunodeficiency virus type 1 integrase: identification of a soluble mutant by systematic replacement of hydrophobic residues., Proceedings of the National Academy of Sciences, vol.92, issue.13, pp.6057-6061, 1995. ,
DOI : 10.1073/pnas.92.13.6057
HIV-1 Integrase Preassembled on Donor DNA Is Refractory to Activity Stimulation by LEDGF/p75, Biochemistry, vol.46, issue.10, pp.2899-2908, 2007. ,
DOI : 10.1021/bi602387u
Efficient and Specific Internal Cleavage of a Retroviral Palindromic DNA Sequence by Tetrameric HIV-1 Integrase, PLoS ONE, vol.66, issue.7, p.608, 2007. ,
DOI : 10.1371/journal.pone.0000608.t001
URL : https://hal.archives-ouvertes.fr/hal-00211177
4 program suite, Acta Crystallographica Section D Biological Crystallography, vol.59, issue.7, pp.1131-1137, 2003. ,
DOI : 10.1107/S0907444903008126
Crystal structures of the catalytic domain of HIV-1 integrase free and complexed with its metal cofactor: high level of similarity of the active site with other viral integrases, Journal of Molecular Biology, vol.282, issue.2, pp.359-368, 1998. ,
DOI : 10.1006/jmbi.1998.2002
5 for the refinement of macromolecular crystal structures, Acta Crystallographica Section D Biological Crystallography, vol.57, issue.4, pp.355-367, 2011. ,
DOI : 10.1107/S0907444911001314
The ARP/WARP suite for automated construction and refinement of protein models The Netherlands: Kluwer Academic, In Int. Tables for Crystallography. Dordrecht, 2001. ,
Fragmentation-Tree Density Representation for Crystallographic Modelling of Bound Ligands, Journal of Molecular Biology, vol.419, issue.3-4, pp.211-222, 2012. ,
DOI : 10.1016/j.jmb.2012.03.012
The PyMOL Molecular Graphics System, 2002. ,