| Literature DB >> 25869309 |
Harish Shukla1, Vikash Kumar1, Amit Kumar Singh1, Shivangi Rastogi2, Shaheb Raj Khan2, Mohammad Imran Siddiqi3, Manju Yasoda Krishnan4, Md Sohail Akhtar5.
Abstract
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 μM. 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 (Kd - 6.68 μM).Entities:
Keywords: Docking; Glyoxylate shunt; Isocitrate lyase; Mycobacteria; Quercetin
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Year: 2015 PMID： 25869309 DOI： 10.1016/j.ijbiomac.2015.04.005
Source DB: PubMed Journal: Int J Biol Macromol ISSN： 0141-8130 Impact factor: 6.953