A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR.
about
Compounds for use in the treatment of mycobacterial infections: a patent evaluation (WO2014049107A1).Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays.A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boostersHarnessing allostery: a novel approach to drug discovery.Protein crystallography and drug discovery: recollections of knowledge exchange between academia and industry.Target Identification of Mycobacterium tuberculosis Phenotypic Hits Using a Concerted Chemogenomic, Biophysical, and Structural Approach.New active leads for tuberculosis booster drugs by structure-based drug discovery.Fragment Screening against the EthR-DNA Interaction by Native Mass Spectrometry.Validating and enabling phosphoglycerate dehydrogenase (PHGDH) as a target for fragment-based drug discovery in PHGDH-amplified breast cancer.Reversing allosteric communication: From detecting allosteric sites to inducing and tuning targeted allosteric response.
P2860
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P2860
A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR.
description
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2014年の論文
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name
A structure-guided fragment-ba ...... of transcription factor EthR.
@ast
A structure-guided fragment-ba ...... of transcription factor EthR.
@en
type
label
A structure-guided fragment-ba ...... of transcription factor EthR.
@ast
A structure-guided fragment-ba ...... of transcription factor EthR.
@en
prefLabel
A structure-guided fragment-ba ...... of transcription factor EthR.
@ast
A structure-guided fragment-ba ...... of transcription factor EthR.
@en
P2093
P2860
P356
P1433
P1476
A structure-guided fragment-ba ...... of transcription factor EthR.
@en
P2093
Benoit Lechartier
Chris Abell
Sachin Surade
Stewart T Cole
Tom L Blundell
P2860
P304
P356
10.1042/BJ20131127
P407
P577
2014-03-01T00:00:00Z