(Q38996602)

8 September 2017

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title

Fragment-based approaches to TB drugs (English)

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8 September 2017

Anthony G Coyne

3

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author name string

Chiara Marchetti

series ordinal

1

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8 September 2017

Daniel S H Chan

series ordinal

2

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8 September 2017

Chris Abell

series ordinal

4

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8 September 2017

publication date

2 November 2016

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8 September 2017

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8 September 2017

page(s)

1-12

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

8 September 2017

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1 reference

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Inhibition ofMycobacterium tuberculosisTransaminase BioA by Aryl Hydrazines and Hydrazides

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

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7 January 2021

Fragment-Based Approaches to the Development of Mycobacterium tuberculosis CYP121 Inhibitors

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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

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7 January 2021

Atomic structure of Mycobacterium tuberculosis CYP121 to 1.06 A reveals novel features of cytochrome P450

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7 January 2021

Studies of the mode of action of amiclenomycin

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7 January 2021

Role of the major antigen of Mycobacterium tuberculosis in cell wall biogenesis

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7 January 2021

Fragment-based discovery of selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase PtpA.

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7 January 2021

Application of fragment screening and merging to the discovery of inhibitors of the Mycobacterium tuberculosis cytochrome P450 CYP121

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7 January 2021

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

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7 January 2021

Mycobacterium tuberculosis cytochrome P450 enzymes: a cohort of novel TB drug targets

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7 January 2021

Biosynthesis of pantothenate

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7 January 2021

Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence

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7 January 2021

Application of fragment growing and fragment linking to the discovery of inhibitors of Mycobacterium tuberculosis pantothenate synthetase

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7 January 2021

Overcoming the Limitations of Fragment Merging: Rescuing a Strained Merged Fragment Series TargetingMycobacterium tuberculosisCYP121

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7 January 2021

Protein tyrosine phosphatases: from genes, to function, to disease

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Identification and structural basis of the reaction catalyzed by CYP121, an essential cytochrome P450 in Mycobacterium tuberculosis

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7 January 2021

Large-scale structural analysis of the classical human protein tyrosine phosphatome

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7 January 2021

Characterization of Active Site Structure in CYP121: A CYTOCHROME P450 ESSENTIAL FOR VIABILITY OF MYCOBACTERIUM TUBERCULOSIS H37Rv

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7 January 2021

Discovery of Mycobacterium tuberculosis protein tyrosine phosphatase B (PtpB) inhibitors from natural products

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7 January 2021

Structural biology in fragment-based drug design

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Disruption of mptpB impairs the ability of Mycobacterium tuberculosis to survive in guinea pigs.

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Coenzyme A biosynthesis: an antimicrobial drug target

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Synthetic EthR inhibitors boost antituberculous activity of ethionamide

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The challenge of new drug discovery for tuberculosis

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7 January 2021

Crystal structures of a pantothenate synthetase fromM. tuberculosisand its complexes with substrates and a reaction intermediate

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7 January 2021

Design and synthesis of potential mechanism-based inhibitors of the aminotransferase BioA involved in biotin biosynthesis.

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7 January 2021

A pantothenate auxotroph of Mycobacterium tuberculosis is highly attenuated and protects mice against tuberculosis.

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7 January 2021

Dynamic substrate enhancement for the identification of specific, second-site-binding fragments targeting a set of protein tyrosine phosphatases.

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7 January 2021

Integrated biophysical approach to fragment screening and validation for fragment-based lead discovery

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7 January 2021

Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches

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7 January 2021

Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB.

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7 January 2021

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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7 January 2021

Recent developments in fragment-based drug discovery

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7 January 2021

High-throughput discovery of Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) inhibitors using click chemistry

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7 January 2021

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

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7 January 2021

A three-stage biophysical screening cascade for fragment-based drug discovery.

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7 January 2021

Evaluating the sensitivity of Mycobacterium tuberculosis to biotin deprivation using regulated gene expression

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7 January 2021

A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters

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7 January 2021

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

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7 January 2021

Inactivation of the antigen 85C gene profoundly affects the mycolate content and alters the permeability of the Mycobacterium tuberculosis cell envelope

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7 January 2021

The antituberculosis drug ethionamide is activated by a flavoprotein monooxygenase

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7 January 2021

Novel small molecule inhibitors of MDR Mycobacterium tuberculosis by NMR fragment screening of antigen 85C.

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7 January 2021

Optimization of Inhibitors of Mycobacterium tuberculosis Pantothenate Synthetase Based on Group Efficiency Analysis

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7 January 2021

Fragment-based approaches in drug discovery and chemical biology

1 reference

https://api.crossref.org/works/10.1017%2FS0031182016001876

7 January 2021

10.1017/S0031182016001876

Identifiers

DOI

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1 reference