(Q35061722)

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A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR.

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Europe PubMed Central

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6 August 2017

A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR. (English)

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Europe PubMed Central

PubMed publication ID

6 August 2017

allosteric inhibitor

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based on heuristic

inferred from title

2

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Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

3

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

5

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Stewart T Cole

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

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Sachin Surade

1

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

Benoit Lechartier

4

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

Chris Abell

6

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

Tom L Blundell

7

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10 June 2020

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1 March 2014

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Europe PubMed Central

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6 August 2017

Biochemical Journal

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

458

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10 June 2020

2

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10 June 2020

387-394

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

Structural biology in fragment-based drug design

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Using a Fragment-Based Approach To Target Protein-Protein Interactions

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Ethionamide activation and sensitivity in multidrug-resistant Mycobacterium tuberculosis

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

The antituberculosis drug ethionamide is activated by a flavoprotein monooxygenase

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Structure of EthR in a ligand bound conformation reveals therapeutic perspectives against tuberculosis

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Crystal structure of the TetR/CamR family repressor Mycobacterium tuberculosis EthR implicated in ethionamide resistance

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Insights into mechanisms of induction and ligands recognition in the transcriptional repressor EthR from Mycobacterium tuberculosis

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Evaluation of fluorescence-based thermal shift assays for hit identification in drug discovery

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

EthR, a repressor of the TetR/CamR family implicated in ethionamide resistance in mycobacteria, octamerizes cooperatively on its operator

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Synthetic EthR inhibitors boost antituberculous activity of ethionamide

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Overview of the CCP4 suite and current developments

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

A graphical user interface to the CCP4 program suite

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

An introduction to data reduction: space-group determination, scaling and intensity statistics

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Phasercrystallographic software

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Refinement of macromolecular structures by the maximum-likelihood method

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Coot: model-building tools for molecular graphics

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Resazurin microtiter assay plate: simple and inexpensive method for detection of drug resistance in Mycobacterium tuberculosis.

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Exploring drug target flexibility using in situ click chemistry: application to a mycobacterial transcriptional regulator

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Molecular recognition of receptor sites using a genetic algorithm with a description of desolvation

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Improved protein-ligand docking using GOLD

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

A complex task? Direct modulation of transcription factors with small molecules

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally po

1 reference

https://api.crossref.org/works/10.1042%2FBJ20131127

21 January 2018

Identifiers

10.1042/BJ20131127

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24313835%20AND%20SRC:MED&resulttype=core&format=json

10 June 2020

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