everolimus has been researched along with Seizures* in 2 studies
2 other study(ies) available for everolimus and Seizures
| Article | Year |
|---|---|
Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.
Recent clinical evaluation of everolimus for seizure reduction in patients with tuberous sclerosis complex (TSC), a disease with overactivated mechanistic target of rapamycin (mTOR) signaling, has demonstrated the therapeutic value of mTOR inhibitors for central nervous system (CNS) indications. Given that everolimus is an incomplete inhibitor of the mTOR function, we sought to develop a new mTOR inhibitor that has improved properties and is suitable for CNS disorders. Starting from an in-house purine-based compound, optimization of the physicochemical properties of a thiazolopyrimidine series led to the discovery of the small molecule Topics: Animals; Anticonvulsants; Binding Sites; Brain; Drug Discovery; Humans; Male; Mice, Inbred C57BL; Mice, Knockout; Neurons; Protein Binding; Protein Kinase Inhibitors; Pyrimidines; Rats; Seizures; Thiazoles; TOR Serine-Threonine Kinases; Tuberous Sclerosis Complex 1 Protein | 2020 |
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.
Topics: Animals; Azabicyclo Compounds; Blood-Brain Barrier; Cell Line, Tumor; Cell Proliferation; Humans; Mechanistic Target of Rapamycin Complex 1; Mechanistic Target of Rapamycin Complex 2; Mice; Models, Molecular; Phosphatidylinositol 3-Kinases; Protein Conformation; Pyridines; Rats; Seizures; Triazines | 2018 |