Structural and Functional Analyses of the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir (S/GSK1349572) (Q27670616)

7

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Stephen H. Hughes

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object named as

Stephen H Hughes

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author name string

Stephen Hare

1

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Steven J Smith

2

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Mathieu Métifiot

3

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Albert Jaxa-Chamiec

The mechanism of retroviral integration from X-ray structures of its key intermediates

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publication date

October 2011

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published in

Molecular Pharmacology

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volume

80

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issue

4

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page(s)

565-72

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cites work

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Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance.

20 March 2017

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Identification of novel mutations responsible for resistance to MK-2048, a second-generation HIV-1 integrase inhibitor

20 March 2017

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Retroviral intasome assembly and inhibition of DNA strand transfer

20 March 2017

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Functional and structural characterization of the integrase from the prototype foamy virus

20 March 2017

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High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations

20 March 2017

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A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera

20 March 2017

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Crystallographic approach to identification of cyclin-dependent kinase 4 (CDK4)-specific inhibitors by using CDK4 mimic CDK2 protein

20 March 2017

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20 March 2017

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Refinement of macromolecular structures by the maximum-likelihood method

20 March 2017

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PRODRG: a tool for high-throughput crystallography of protein-ligand complexes

20 March 2017

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Remarks about protein structure precision

20 March 2017

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Structure-based modeling of the functional HIV-1 intasome and its inhibition

20 March 2017

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Resistance to integrase inhibitors

29 September 2017

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Primary mutations selected in vitro with raltegravir confer large fold changes in susceptibility to first-generation integrase inhibitors, but minor fold changes to inhibitors with second-generation resistance profiles

29 September 2017

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

29 September 2017

1 reference

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HIV-1 IN inhibitors: 2010 update and perspectives

29 September 2017

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

29 September 2017

1 reference

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Drug resistance profiles for the HIV integrase gene in patients failing raltegravir salvage therapy

29 September 2017

1 reference

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

29 September 2017

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2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one-based HIV-1 integrase inhibitors

29 September 2017

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Novel HIV-1 integrase inhibitors derived from quinolone antibiotics

29 September 2017

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Retroviral DNA integration: reaction pathway and critical intermediates

29 September 2017

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

29 September 2017

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

29 September 2017

1 reference

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Objective comparison of protein structures: error-scaled difference distance matrices

29 September 2017

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Identification of conserved amino acid residues critical for human immunodeficiency virus type 1 integrase function in vitro

29 September 2017

1 reference

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Residues critical for retroviral integrative recombination in a region that is highly conserved among retroviral/retrotransposon integrases and bacterial insertion sequence transposases

29 September 2017

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Elvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143.

29 September 2017

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In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor

2 June 2018

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Cross-resistance profile determination of two second-generation HIV-1 integrase inhibitors using a panel of recombinant viruses derived from raltegravir-treated clinical isolates

2 June 2018

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LEDGF/p75 interacts with divergent lentiviral integrases and modulates their enzymatic activity in vitro

2 June 2018

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The terminal (catalytic) adenosine of the HIV LTR controls the kinetics of binding and dissociation of HIV integrase strand transfer inhibitors

2 June 2018

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

27 November 2018

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Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection

27 November 2018

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Structure-based optimization of novel azepane derivatives as PKB inhibitors

27 November 2018

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27 November 2018

Identifiers

DOI

10.1124/MOL.111.073189

1 reference

1 reference

1 reference

PubMed publication ID

21719464

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