The LEDGF/p75 integrase interaction, a novel target for anti-HIV therapy (Q26849265)

language of work or name

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5 January 2013

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435

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PubMed

issue

1

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PubMed

page(s)

102-9

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Inhibitory profile of a LEDGF/p75 peptide against HIV-1 integrase: insight into integrase-DNA complex formation and catalysis

PubMed

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

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Lens epithelium-derived growth factor/p75 interacts with the transposase-derived DDE domain of PogZ.

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Identification of the LEDGF/p75 binding site in HIV-1 integrase

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HIV-1 integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells

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Identification of an evolutionarily conserved domain in human lens epithelium-derived growth factor/transcriptional co-activator p75 (LEDGF/p75) that binds HIV-1 integrase

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Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75.

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Solution structure of the HIV-1 integrase-binding domain in LEDGF/p75

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Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization

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Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication

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A role for LEDGF/p75 in targeting HIV DNA integration

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A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series

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

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HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation

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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

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Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication

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Phage display-directed discovery of LEDGF/p75 binding cyclic peptide inhibitors of HIV replication.

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D77, one benzoic acid derivative, functions as a novel anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75.

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Integrase mutants defective for interaction with LEDGF/p75 are impaired in chromosome tethering and HIV-1 replication

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HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase

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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

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Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy

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LEDGF/p75: a novel nuclear autoantigen at the crossroads of cell survival and apoptosis

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Resistance associated mutations to dolutegravir (S/GSK1349572) in HIV-infected patients--impact of HIV subtypes and prior raltegravir experience.

7 January 2021

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Isolation of cDNAs encoding novel transcription coactivators p52 and p75 reveals an alternate regulatory mechanism of transcriptional activation

7 January 2021

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Role of the PWWP domain of lens epithelium-derived growth factor (LEDGF)/p75 cofactor in lentiviral integration targeting

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Retroviral intasome assembly and inhibition of DNA strand transfer

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Cyclic peptide inhibitors of HIV-1 integrase derived from the LEDGF/p75 protein

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Mechanism of action of the HIV-1 integrase inhibitory peptide LEDGF 361-370.

7 January 2021

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Inhibiting HIV-1 integrase by shifting its oligomerization equilibrium

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The transcriptional co-activator LEDGF/p75 displays a dynamic scan-and-lock mechanism for chromatin tethering

7 January 2021

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Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV.

7 January 2021

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Selection of human immunodeficiency virus type 1 resistance against the pyranodipyrimidine V-165 points to a multimodal mechanism of action.

7 January 2021

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

7 January 2021

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Identification of old drugs as potential inhibitors of HIV-1 integrase - human LEDGF/p75 interaction via molecular docking

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Hepatoma-derived growth factor belongs to a gene family in mice showing significant homology in the amino terminus

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Multimode, Cooperative Mechanism of Action of Allosteric HIV-1 Integrase Inhibitors

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FRET analysis reveals distinct conformations of IN tetramers in the presence of viral DNA or LEDGF/p75.

7 January 2021

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Lens epithelium-derived growth factor/p75 prevents proteasomal degradation of HIV-1 integrase

7 January 2021

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An essential role for LEDGF/p75 in HIV integration

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Identification and characterization of the chromatin-binding domains of the HIV-1 integrase interactor LEDGF/p75.

7 January 2021

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LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in human cells

7 January 2021

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Transcriptional co-activator p75 binds and tethers the Myc-interacting protein JPO2 to chromatin

7 January 2021

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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

7 January 2021

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Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro

7 January 2021

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Role of PSIP1/LEDGF/p75 in lentiviral infectivity and integration targeting

7 January 2021

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In vitro DNA tethering of HIV-1 integrase by the transcriptional coactivator LEDGF/p75.

7 January 2021

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Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults

7 January 2021

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Identification of a small-molecule binding site at the dimer interface of the HIV integrase catalytic domain

7 January 2021

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Antiretroviral therapy with the integrase inhibitor raltegravir alters decay kinetics of HIV, significantly reducing the second phase

7 January 2021

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Spatial and temporal dynamics of two alternatively spliced regulatory factors, lens epithelium-derived growth factor (ledgf/p75) and p52, in the nucleus

7 January 2021

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Small Molecule Inhibitors of the LEDGF Site of Human Immunodeficiency Virus Integrase Identified by Fragment Screening and Structure Based Design

7 January 2021

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

7 January 2021

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LEDGF/p75-independent HIV-1 replication demonstrates a role for HRP-2 and remains sensitive to inhibition by LEDGINs

7 January 2021

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Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137)

7 January 2021

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Wild-type levels of human immunodeficiency virus type 1 infectivity in the absence of cellular emerin protein

7 January 2021

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LEDGF/p75 functions downstream from preintegration complex formation to effect gene-specific HIV-1 integration

7 January 2021

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Lens epithelium-derived growth factor (LEDGF/p75) and p52 are derived from a single gene by alternative splicing

7 January 2021

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Lens epithelium-derived growth factor: effects on growth and survival of lens epithelial cells, keratinocytes, and fibroblasts

7 January 2021

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The PWWP domain: a potential protein-protein interaction domain in nuclear proteins influencing differentiation?

7 January 2021

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Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection

7 January 2021

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New Class of HIV-1 Integrase (IN) Inhibitors with a Dual Mode of Action

7 January 2021

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Nuclear protein LEDGF/p75 recognizes supercoiled DNA by a novel DNA-binding domain

7 January 2021

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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

7 January 2021

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Cellular co-factors of HIV-1 integration

7 January 2021

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Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodeficiency virus

7 January 2021

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Menin critically links MLL proteins with LEDGF on cancer-associated target genes

7 January 2021

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Activity of elvitegravir, a once-daily integrase inhibitor, against resistant HIV Type 1: results of a phase 2, randomized, controlled, dose-ranging clinical trial

7 January 2021

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