Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor (Q33797858)

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English	Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor	scientific article

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scholarly article

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Europe PubMed Central

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29 July 2017

Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor (English)

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29 July 2017

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Paul Edwards

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29 July 2017

Michael G Cordingley

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object named as

Michael Cordingley

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29 July 2017

Anne-Marie Faucher

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Anne-Marie Faucher

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29 July 2017

1

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Craig Fenwick

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29 July 2017

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Ma'an Amad

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29 July 2017

Murray D Bailey

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29 July 2017

Richard Bethell

4

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Michael Bös

5

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Pierre Bonneau

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29 July 2017

René Coulombe

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29 July 2017

Jianmin Duan

9

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Lee D Fader

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29 July 2017

Michel Garneau

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Araz Jakalian

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Stephen Kawai

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Louie Lamorte

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Steven LaPlante

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Laibin Luo

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29 July 2017

Steve Mason

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29 July 2017

Marc-André Poupart

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29 July 2017

Nathalie Rioux

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Patricia Schroeder

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29 July 2017

Bruno Simoneau

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29 July 2017

Sonia Tremblay

24

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29 July 2017

Youla Tsantrizos

25

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29 July 2017

Myriam Witvrouw

26

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29 July 2017

Christiane Yoakim

27

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29 July 2017

language of work or name

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publication date

24 March 2014

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29 July 2017

Antimicrobial Agents and Chemotherapy

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29 July 2017

58

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6

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29 July 2017

3233-3244

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29 July 2017

Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Allosteric inhibition of HIV-1 integrase activity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

The importance of plasma protein binding in drug discovery

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Distinct Effects of Two HIV-1 Capsid Assembly Inhibitor Families That Bind the Same Site within the N-Terminal Domain of the Viral CA Protein

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Preclinical Characterization of BI 201335, a C-Terminal Carboxylic Acid Inhibitor of the Hepatitis C Virus NS3-NS4A Protease

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

5th International AIDS Society Conference on HIV Pathogenesis, Treatment and Prevention: summary of key research and implications for policy and practice - clinical sciences

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Biochemical and pharmacological analyses of HIV-1 integrase flexible loop mutants resistant to raltegravir

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Retroviral intasome assembly and inhibition of DNA strand transfer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Elvitegravir: a new HIV integrase inhibitor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

HIV type 1 integrase inhibitors: from basic research to clinical implications

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Resistance mutations in human immunodeficiency virus type 1 integrase selected with elvitegravir confer reduced susceptibility to a wide range of integrase inhibitors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Dose-response curve slope sets class-specific limits on inhibitory potential of anti-HIV drugs

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Potential for new antiretrovirals to address unmet needs in the management of HIV-1 infection.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Integrase, LEDGF/p75 and HIV replication

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

LEDGF/p75 determines cellular trafficking of diverse lentiviral but not murine oncoretroviral integrase proteins and is a component of functional lentiviral preintegration complexes

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Integrase-specific enhancement and suppression of retroviral DNA integration by compacted chromatin structure in vitro

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

HIV-1 integrase: structural organization, conformational changes, and catalysis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Human serum attenuates the activity of protease inhibitors toward wild-type and mutant human immunodeficiency virus

1 reference

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28 July 2018

HIV-1-induced cell fusion is mediated by multiple regions within both the viral envelope and the CCR-5 co-receptor

1 reference

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28 July 2018

Second locus involved in human immunodeficiency virus type 1 resistance to protease inhibitors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4068430

28 July 2018

Incorporation of a fluorescent guanosine analog into oligonucleotides and its application to a real time assay for the HIV-1 integrase 3'-processing reaction

1 reference

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28 July 2018

Rapid colorimetric assay for cellular growth and survival: Application to proliferation and cytotoxicity assays

1 reference

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28 July 2018

Production of acquired immunodeficiency syndrome-associated retrovirus in human and nonhuman cells transfected with an infectious molecular clone

1 reference

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28 July 2018

Significance of "extravascular" protein binding for antimicrobial pharmacodynamics in an in vitro capillary model of infection

1 reference

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A three-dimensional model to analyze drug-drug interactions

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Three-dimensional analysis of the synergistic cytotoxicity of ganciclovir and zidovudine

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Activities of human immunodeficiency virus (HIV) integration protein in vitro: specific cleavage and integration of HIV DNA

1 reference

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Identification and characterization of a novel HIV-1 nucleotide-competing reverse transcriptase inhibitor series

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30 October 2018

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30 October 2018

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

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30 October 2018

New hexahydrodiazocino-naphthyridine triones as HIV-1 integrase inhibitors: WO2008048538 A1.

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30 October 2018

Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants

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30 October 2018

An essential role for LEDGF/p75 in HIV integration

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30 October 2018

Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes

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Use of homogeneous time-resolved fluorescence energy transfer in the measurement of nuclear receptor activation

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30 October 2018

Identifiers

10.1128/AAC.02719-13

1 reference

Europe PubMed Central

PubMed publication ID

29 July 2017

PMC publication ID

1 reference

Europe PubMed Central

PubMed publication ID

29 July 2017

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

29 July 2017

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