LEDGINs, non-catalytic site inhibitors of HIV-1 integrase: a patent review (2006 - 2014). (Q38199193)

30 August 2017

title

LEDGINs, non-catalytic site inhibitors of HIV-1 integrase: a patent review (2006 - 2014). (English)

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30 August 2017

5

Zeger Debyser

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Jonas Demeulemeester

object named as

Jonas Demeulemeester

series ordinal

1

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Marc De Maeyer

series ordinal

4

object named as

Marc De Maeyer

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30 August 2017

6

Frauke Christ

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30 August 2017

Patrick Chaltin

2

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30 August 2017

Arnaud Marchand

series ordinal

3

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30 August 2017

language of work or name

English

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publication date

25 March 2014

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Expert Opinion on Therapeutic Patents

30 August 2017

published in

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30 August 2017

volume

24

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30 August 2017

issue

6

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30 August 2017

page(s)

609-632

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The structural biology of HIV-1: mechanistic and therapeutic insights

30 August 2017

cites work

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Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells

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The development of novel HIV integrase inhibitors and the problem of drug resistance.

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Allosteric inhibitor development targeting HIV-1 integrase

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In search of second-generation HIV integrase inhibitors: targeting integration beyond strand transfer

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Allosteric inhibition of HIV-1 integrase activity

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

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

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

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Structural basis for high-affinity binding of LEDGF PWWP to mononucleosomes

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Nucleosomal DNA binding drives the recognition of H3K36-methylated nucleosomes by the PSIP1-PWWP domain

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

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Identification and characterization of a functional nuclear localization signal in the HIV-1 integrase interactor LEDGF/p75

21 January 2018

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

21 January 2018

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High-resolution profiling of the LEDGF/p75 chromatin interaction in the ENCODE region

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

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

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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

21 January 2018

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A role for LEDGF/p75 in targeting HIV DNA integration

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

21 January 2018

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

21 January 2018

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LEDGF/p75 interferes with the formation of synaptic nucleoprotein complexes that catalyze full-site HIV-1 DNA integration in vitro: implications for the mechanism of viral cDNA integration

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

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

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

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Inhibiting HIV-1 integrase by shifting its oligomerization equilibrium

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

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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.

21 January 2018

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

21 January 2018

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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

21 January 2018

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

21 January 2018

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

21 January 2018

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

21 January 2018

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

21 January 2018

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The osmium-catalyzed asymmetric dihydroxylation: a new ligand class and a process improvement

21 January 2018

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Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds

21 January 2018

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An essential role for LEDGF/p75 in HIV integration

21 January 2018

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Multiple dendritic catalysts for asymmetric transfer hydrogenation

21 January 2018

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

21 January 2018

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Fragment-based discovery of 8-hydroxyquinoline inhibitors of the HIV-1 integrase-lens epithelium-derived growth factor/p75 (IN-LEDGF/p75) interaction

21 January 2018

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Discovery of inhibitors to block interactions of HIV-1 integrase with human LEDGF/p75 via structure-based virtual screening and bioassays.

21 January 2018

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Discovery of novel inhibitors of LEDGF/p75-IN protein-protein interactions

21 January 2018

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Structural basis for a new mechanism of inhibition of HIV-1 integrase identified by fragment screening and structure-based design

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2014.898753

The A128T Resistance Mutation Reveals Aberrant Protein Multimerization as the Primary Mechanism of Action of Allosteric HIV-1 Integrase Inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Dynamic modulation of HIV-1 integrase structure and function by cellular lens epithelium-derived growth factor (LEDGF) protein

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Characterization of rare lens epithelium-derived growth factor/p75 genetic variants identified in HIV-1 long-term nonprogressors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Dual inhibition of HIV-1 replication by integrase-LEDGF allosteric inhibitors is predominant at the post-integration stage

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Development of an AlphaScreen-based HIV-1 integrase dimerization assay for discovery of novel allosteric inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Dithiothreitol causes HIV-1 integrase dimer dissociation while agents interacting with the integrase dimer interface promote dimer formation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

LEDGINs inhibit late stage HIV-1 replication by modulating integrase multimerization in the virions

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Non-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Multimodal mechanism of action of allosteric HIV-1 integrase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2014.898753

A critical subset model provides a conceptual basis for the high antiviral activity of major HIV drugs

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Clinical use of HIV integrase inhibitors: a systematic review and meta-analysis

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2014.898753

Safety and efficacy of dolutegravir in treatment-experienced subjects with raltegravir-resistant HIV type 1 infection: 24-week results of the VIKING Study

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2014.898753

10.1517/13543776.2014.898753

21 January 2018

Identifiers

DOI

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30 August 2017

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