Journal
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Volume 78, Issue -, Pages 137-141Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijbiomac.2015.04.005
Keywords
Isocitrate lyase; Quercetin; Glyoxylate shunt; Mycobacteria; Docking
Funding
- CSIR-UNDO [BSC0103]
- CSIR-GENESIS [BSC0121]
- CSIR
- DBT, New Delhi
- [CSIR-YSA001]
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Combating tuberculosis requires new therapeutic strategies that not only target the actively dividing bacilli but also the dormant bacilli during persistent infection. Isocitrate lyase (ICL) is a key enzyme of the glyoxylate shunt, crucial for the survival of bacteria in macrophages and mice. MtbICL is considered as one of the potential and attractive drug targets against persistent infection. We report the inhibition of MtbICL by quercetin with IC50 of 3.57 mu M. In addition, quercetin strongly inhibited the growth of Mtb H37Rv utilizing acetate, rather than glucose as the sole carbon source, suggesting the inhibition of glyoxylate shunt. Quercetin binds at the N-terminus of MtbICL (K-d - 6.68 mu M). (C) 2015 Elsevier B.V. All rights reserved.
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