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Development of NMR and thermal shift assays for the evaluation of Mycobacterium tuberculosis isocitrate lyase inhibitors.

Reynisson

Development of NMR and thermal shift assays for the evaluation of Mycobacterium tuberculosis isocitrate lyase inhibitors. Thumbnail


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Abstract

The enzymes isocitrate lyase (ICL) isoforms 1 and 2 are essential for Mycobacterium tuberculosis survival within macrophages during latent tuberculosis (TB). As such, ICLs are attractive therapeutic targets for the treatment of tuberculosis. However, there are few biophysical assays that are available for accurate kinetic and inhibition studies of ICL in vitro. Herein we report the development of a combined NMR spectroscopy and thermal shift assay to study ICL inhibitors for both screening and inhibition constant (IC50) measurement. Operating this new assay in tandem with virtual high-throughput screening has led to the discovery of several new ICL1 inhibitors.

Citation

Reynisson. (2017). Development of NMR and thermal shift assays for the evaluation of Mycobacterium tuberculosis isocitrate lyase inhibitors. MedChemComm, 2155 - 2163. https://doi.org/10.1039/c7md00456g

Acceptance Date Oct 16, 2017
Publication Date Oct 17, 2017
Journal MedChemComm
Print ISSN 2040-2503
Publisher Royal Society of Chemistry
Pages 2155 - 2163
DOI https://doi.org/10.1039/c7md00456g
Keywords tuberculosis
Publisher URL https://pubs.rsc.org/en/Content/ArticleLanding/2017/MD/C7MD00456G#!divAbstract

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