Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands.

Published in: Nucleic Acids Res., 2012 vol. 40(7) pp. 3018-30

By: Carette X et al.


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.

Published in: J. Med. Chem., 2012 vol. 55(1) pp. 68-83

By: Flipo M et al.


MALDI imaging techniques dedicated to drug-distribution studies.

Published in: Bioanalysis, 2011 vol. 3(12) pp. 1399-406

By: Bonnel D et al.


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

Published in: J. Med. Chem., 2011 vol. 54(8) pp. 2994-3010

By: Flipo M et al.


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

Published in: ACS Chem. Biol., 2010 vol. 5(11) pp. 1007-13

By: Willand N et al.


Synthetic EthR inhibitors boost antituberculous activity of ethionamide.

Published in: Nat. Med., 2009 vol. 15(5) pp. 537-44

By: Willand N et al.


A synthetic mammalian gene circuit reveals antituberculosis compounds.

Published in: Proc Natl Acad Sci U S A. 2008 Jul 22;105(29):9994-8. doi: 10.1073/pnas.0800663105. Epub 2008 Jul 9

By: Weber W et al.


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

Published in: Mol Cell. 2004 Oct 22;16(2):301-7

By: Frénois F et al.

Video

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

Published in: Mol Microbiol. 2004 Jan;51(1):175-88

By: Engohang-Ndong J et al.

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