Functional drug screening reveals anticonvulsants as enhancers of mTOR-independent autophagic killing of Mycobacterium tuberculosis through inositol depletion.

Mark Schiebler; Karen Brown; Krisztina Hegyi; Sandra M Newton; Maurizio Renna; Lucy Hepburn; Catherine Klapholz; Sarah Coulter; Andres Obregón-Henao; Marcela Henao Tamayo; +12 more... Randall Basaraba; Beate Kampmann ORCID logo; Katherine M Henry; Joseph Burgon; Stephen A Renshaw; Angeleen Fleming; Robert R Kay; Karen E Anderson; Phillip T Hawkins; Diane J Ordway; David C Rubinsztein; Rodrigo Andres Floto; (2015) Functional drug screening reveals anticonvulsants as enhancers of mTOR-independent autophagic killing of Mycobacterium tuberculosis through inositol depletion. EMBO MOLECULAR MEDICINE, 7 (2). pp. 127-139. ISSN 1757-4676 DOI: 10.15252/emmm.201404137
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Mycobacterium tuberculosis (MTB) remains a major challenge to global health made worse by the spread of multidrug resistance. We therefore examined whether stimulating intracellular killing of mycobacteria through pharmacological enhancement of macroautophagy might provide a novel therapeutic strategy. Despite the resistance of MTB to killing by basal autophagy, cell-based screening of FDA-approved drugs revealed two anticonvulsants, carbamazepine and valproic acid, that were able to stimulate autophagic killing of intracellular M. tuberculosis within primary human macrophages at concentrations achievable in humans. Using a zebrafish model, we show that carbamazepine can stimulate autophagy in vivo and enhance clearance of M. marinum, while in mice infected with a highly virulent multidrug-resistant MTB strain, carbamazepine treatment reduced bacterial burden, improved lung pathology and stimulated adaptive immunity. We show that carbamazepine induces antimicrobial autophagy through a novel, evolutionarily conserved, mTOR-independent pathway controlled by cellular depletion of myo-inositol. While strain-specific differences in susceptibility to in vivo carbamazepine treatment may exist, autophagy enhancement by repurposed drugs provides an easily implementable potential therapy for the treatment of multidrug-resistant mycobacterial infection.


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