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

[1]  M. Humbert,et al.  Phage display-directed discovery of LEDGF/p75 binding cyclic peptide inhibitors of HIV replication. , 2012, Molecular therapy : the journal of the American Society of Gene Therapy.

[2]  Thomas S. Peat,et al.  Small Molecule Inhibitors of the LEDGF Site of Human Immunodeficiency Virus Integrase Identified by Fragment Screening and Structure Based Design , 2012, PloS one.

[3]  Guixia Liu,et al.  Identification of old drugs as potential inhibitors of HIV-1 integrase – human LEDGF/p75 interaction via molecular docking , 2012, Journal of Molecular Modeling.

[4]  Stephen M. Shaw,et al.  Small-Molecule Inhibitors of the LEDGF/p75 Binding Site of Integrase Block HIV Replication and Modulate Integrase Multimerization , 2012, Antimicrobial Agents and Chemotherapy.

[5]  Xiaohong Liu,et al.  New Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action , 2012, The Journal of Biological Chemistry.

[6]  A. Engelman,et al.  Multimode, Cooperative Mechanism of Action of Allosteric HIV-1 Integrase Inhibitors* , 2012, The Journal of Biological Chemistry.

[7]  F. Bushman,et al.  LEDGF/p75-Independent HIV-1 Replication Demonstrates a Role for HRP-2 and Remains Sensitive to Inhibition by LEDGINs , 2012, PLoS pathogens.

[8]  J. Newman,et al.  Crystal Structures of Novel Allosteric Peptide Inhibitors of HIV Integrase Identify New Interactions at the LEDGF Binding Site , 2011, Chembiochem : a European journal of chemical biology.

[9]  F. Bushman,et al.  Role of the PWWP Domain of Lens Epithelium-derived Growth Factor (LEDGF)/p75 Cofactor in Lentiviral Integration Targeting* , 2011, The Journal of Biological Chemistry.

[10]  Zeger Debyser,et al.  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. , 2011, Antiviral research.

[11]  S. Piscitelli,et al.  Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults , 2011, AIDS.

[12]  N. Neamati,et al.  Design of HIV-1 integrase inhibitors targeting the catalytic domain as well as its interaction with LEDGF/p75: a scaffold hopping approach using salicylate and catechol groups. , 2011, Bioorganic & medicinal chemistry.

[13]  Jelle Hendrix,et al.  In vitro DNA tethering of HIV-1 integrase by the transcriptional coactivator LEDGF/p75. , 2011, Journal of molecular biology.

[14]  K. Musier-Forsyth,et al.  FRET analysis reveals distinct conformations of IN tetramers in the presence of viral DNA or LEDGF/p75 , 2011, Nucleic acids research.

[15]  V. Soriano,et al.  Resistance associated mutations to dolutegravir (S/GSK1349572) in HIV-infected patients--impact of HIV subtypes and prior raltegravir experience. , 2011, Antiviral research.

[16]  T. Miyamoto,et al.  Nuclear protein LEDGF/p75 recognizes supercoiled DNA by a novel DNA-binding domain , 2011, Nucleic acids research.

[17]  Z. Debyser,et al.  HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation. , 2011, European journal of medicinal chemistry.

[18]  H. Benyamini,et al.  Cyclic peptide inhibitors of HIV-1 integrase derived from the LEDGF/p75 protein. , 2010, Bioorganic & medicinal chemistry.

[19]  J. Hofkens,et al.  The transcriptional co-activator LEDGF/p75 displays a dynamic scan-and-lock mechanism for chromatin tethering , 2010, Nucleic acids research.

[20]  A. Marchand,et al.  Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication. , 2010, Nature chemical biology.

[21]  Zvi Hayouka,et al.  Mechanism of action of the HIV-1 integrase inhibitory peptide LEDGF 361-370. , 2010, Biochemical and biophysical research communications.

[22]  A. Zolopa,et al.  Activity of elvitegravir, a once-daily integrase inhibitor, against resistant HIV Type 1: results of a phase 2, randomized, controlled, dose-ranging clinical trial. , 2010, The Journal of infectious diseases.

[23]  A. Engelman,et al.  Retroviral intasome assembly and inhibition of DNA strand transfer , 2010, Nature.

[24]  F. Baldanti,et al.  Early emergence of raltegravir resistance mutations in patients receiving HAART salvage regimens , 2010, Journal of medical virology.

[25]  Z. Debyser,et al.  Pharmacophore‐Based Discovery of Small‐Molecule Inhibitors of Protein–Protein Interactions between HIV‐1 Integrase and Cellular Cofactor LEDGF/p75 , 2009, ChemMedChem.

[26]  J. Rain,et al.  Lens Epithelium-derived Growth Factor/p75 Interacts with the Transposase-derived DDE Domain of PogZ* , 2009, Journal of Biological Chemistry.

[27]  Hualiang Jiang,et al.  D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. , 2008, Biochemical and biophysical research communications.

[28]  D. Hazuda,et al.  Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. , 2008, Journal of medicinal chemistry.

[29]  Akihiko Yokoyama,et al.  Menin critically links MLL proteins with LEDGF on cancer-associated target genes. , 2008, Cancer cell.

[30]  J. Howe,et al.  Screening for Antiviral Inhibitors of the HIV Integrase—LEDGF/p75 Interaction Using the AlphaScreen™ Luminescent Proximity Assay , 2008, Journal of biomolecular screening.

[31]  Myriam Witvrouw,et al.  A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series. , 2008, Bioorganic & medicinal chemistry letters.

[32]  Zeger Debyser,et al.  Inhibitory profile of a LEDGF/p75 peptide against HIV‐1 integrase: Insight into integrase–DNA complex formation and catalysis , 2008, FEBS letters.

[33]  Luba Tchertanov,et al.  Mutations Associated with Failure of Raltegravir Treatment Affect Integrase Sensitivity to the Inhibitor In Vitro , 2008, Antimicrobial Agents and Chemotherapy.

[34]  F. Bushman,et al.  Role of PSIP1/LEDGF/p75 in Lentiviral Infectivity and Integration Targeting , 2007, PloS one.

[35]  D. Hazuda,et al.  Antiretroviral therapy with the integrase inhibitor raltegravir alters decay kinetics of HIV, significantly reducing the second phase , 2007, AIDS.

[36]  M. Matsuoka,et al.  Broad Antiretroviral Activity and Resistance Profile of the Novel Human Immunodeficiency Virus Integrase Inhibitor Elvitegravir (JTK-303/GS-9137) , 2007, Journal of Virology.

[37]  R. Benarous,et al.  Differential interaction of HIV-1 integrase and JPO2 with the C terminus of LEDGF/p75. , 2007, Journal of molecular biology.

[38]  A. Engelman,et al.  LEDGF/p75 functions downstream from preintegration complex formation to effect gene-specific HIV-1 integration. , 2007, Genes & development.

[39]  J. Vercammen,et al.  Selection of human immunodeficiency virus type 1 resistance against the pyranodipyrimidine V-165 points to a multimodal mechanism of action. , 2007, The Journal of antimicrobial chemotherapy.

[40]  Joseph Rosenbluh,et al.  Inhibiting HIV-1 integrase by shifting its oligomerization equilibrium , 2007, Proceedings of the National Academy of Sciences.

[41]  Myriam Witvrouw,et al.  Virus Evolution Reveals an Exclusive Role for LEDGF/p75 in Chromosomal Tethering of HIV , 2007, PLoS pathogens.

[42]  J. Rain,et al.  Identification of the LEDGF/p75 binding site in HIV-1 integrase. , 2007, Journal of molecular biology.

[43]  Wulin Teo,et al.  An Essential Role for LEDGF/p75 in HIV Integration , 2006, Science.

[44]  A. Engelman,et al.  Wild-Type Levels of Human Immunodeficiency Virus Type 1 Infectivity in the Absence of Cellular Emerin Protein , 2006, Journal of Virology.

[45]  Jelle Hendrix,et al.  Overexpression of the Lens Epithelium-Derived Growth Factor/p75 Integrase Binding Domain Inhibits Human Immunodeficiency Virus Replication , 2006, Journal of Virology.

[46]  M. Llano,et al.  Identification and characterization of the chromatin-binding domains of the HIV-1 integrase interactor LEDGF/p75. , 2006, Journal of molecular biology.

[47]  A. Engelman,et al.  Transcriptional co-activator p75 binds and tethers the Myc-interacting protein JPO2 to chromatin , 2006, Journal of Cell Science.

[48]  A. Engelman,et al.  A tripartite DNA-binding element, comprised of the nuclear localization signal and two AT-hook motifs, mediates the association of LEDGF/p75 with chromatin in vivo , 2006, Nucleic acids research.

[49]  C. Van den Haute,et al.  Transient and Stable Knockdown of the Integrase Cofactor LEDGF/p75 Reveals Its Role in the Replication Cycle of Human Immunodeficiency Virus , 2006, Journal of Virology.

[50]  Z. Debyser,et al.  Cellular co-factors of HIV-1 integration. , 2006, Trends in biochemical sciences.

[51]  Paul Shinn,et al.  A role for LEDGF/p75 in targeting HIV DNA integration , 2005, Nature Medicine.

[52]  A. Engelman,et al.  Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75. , 2005, Proceedings of the National Academy of Sciences of the United States of America.

[53]  Myriam Witvrouw,et al.  Integrase Mutants Defective for Interaction with LEDGF/p75 Are Impaired in Chromosome Tethering and HIV-1 Replication* , 2005, Journal of Biological Chemistry.

[54]  A. Engelman,et al.  Solution structure of the HIV-1 integrase-binding domain in LEDGF/p75 , 2005, Nature Structural &Molecular Biology.

[55]  M. Llano,et al.  Lens Epithelium-derived Growth Factor/p75 Prevents Proteasomal Degradation of HIV-1 Integrase* , 2004, Journal of Biological Chemistry.

[56]  Pamela A. Silver,et al.  Identification of an Evolutionarily Conserved Domain in Human Lens Epithelium-derived Growth Factor/Transcriptional Co-activator p75 (LEDGF/p75) That Binds HIV-1 Integrase* , 2004, Journal of Biological Chemistry.

[57]  Matthew P. Repasky,et al.  Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy. , 2004, Journal of medicinal chemistry.

[58]  T. Daniels,et al.  LEDGF/p75: a novel nuclear autoantigen at the crossroads of cell survival and apoptosis. , 2003, Autoimmunity reviews.

[59]  E. De Clercq,et al.  LEDGF/p75 Is Essential for Nuclear and Chromosomal Targeting of HIV-1 Integrase in Human Cells* , 2003, Journal of Biological Chemistry.

[60]  Zeger Debyser,et al.  HIV-1 Integrase Forms Stable Tetramers and Associates with LEDGF/p75 Protein in Human Cells* , 2003, The Journal of Biological Chemistry.

[61]  Frank Dietz,et al.  The family of hepatoma-derived growth factor proteins: characterization of a new member HRP-4 and classification of its subfamilies. , 2002, The Biochemical journal.

[62]  L. Chylack,et al.  Spatial and temporal dynamics of two alternatively spliced regulatory factors, lens epithelium-derived growth factor (ledgf/p75) and p52, in the nucleus , 2001, Cell and Tissue Research.

[63]  F. Bushman,et al.  Identification of a small-molecule binding site at the dimer interface of the HIV integrase catalytic domain. , 2001, Acta crystallographica. Section D, Biological crystallography.

[64]  Amy S. Espeseth,et al.  HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase. , 2000, Proceedings of the National Academy of Sciences of the United States of America.

[65]  J. D. den Dunnen,et al.  The PWWP domain: a potential protein–protein interaction domain in nuclear proteins influencing differentiation? , 2000, FEBS letters.

[66]  L. Chylack,et al.  Lens epithelium-derived growth factor (LEDGF/p75) and p52 are derived from a single gene by alternative splicing. , 2000, Gene.

[67]  L. Chylack,et al.  Lens epithelium-derived growth factor: effects on growth and survival of lens epithelial cells, keratinocytes, and fibroblasts. , 2000, Biochemical and biophysical research communications.

[68]  R. Roeder,et al.  Isolation of cDNAs encoding novel transcription coactivators p52 and p75 reveals an alternate regulatory mechanism of transcriptional activation , 1998, The EMBO journal.

[69]  D. Landsman,et al.  AT-hook motifs identified in a wide variety of DNA-binding proteins. , 1998, Nucleic acids research.

[70]  V. Mikol,et al.  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. , 1998, Journal of molecular biology.

[71]  Hideji Nakamura,et al.  Hepatoma-derived growth factor belongs to a gene family in mice showing significant homology in the amino terminus. , 1997, Biochemical and biophysical research communications.