The novel, catalytic mTORC1/2 inhibitor PQR620 and the PI3K/mTORC1/2 inhibitor PQR530 effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy

Author:

Brandt Claudia,Hillmann Petra,Noack Andreas,Römermann Kerstin,Öhler Leon A.,Rageot Denise,Beaufils Florent,Melone Anna,Sele Alexander M.,Wymann Matthias P.,Fabbro Doriano,Löscher Wolfgang

Funder

Epilepsy Foundation

Publisher

Elsevier BV

Subject

Cellular and Molecular Neuroscience,Pharmacology

Reference79 articles.

1. TORC1-dependent epilepsy caused by acute biallelic Tsc1 deletion in adult mice;Abs;Ann. Neurol.,2013

2. Evidence for the interaction of brainstem systems mediating seizure expression in kindling and electroconvulsive shock seizure models;Applegate;Epilepsy Res.,1991

3. Pilocarpine-induced epilepsy in mice alters seizure thresholds and the efficacy of antiepileptic drugs in the 6-Hertz psychomotor seizure model;Bankstahl;Epilepsy Res.,2013

4. Pharmacological characterization of the selective, orally bioavailable, potent mTORC1/2 inhibitor PQR620;Beaufils,2016

5. Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor;Beaufils,2016

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