期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 12, 页码 4072-4074出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.04.076
关键词
Anticonvulant; Epilepsy; Sweetener; T1R3; Virtual screening; Knowledge-based drug repurposing
资金
- UNLP [Incentivos X-597]
- CONICET [PIP 11220090100603]
- ANPCyT [PICTs 2010-2531, 2010-1774]
A virtual screening campaign based on application of a topological discriminant function capable of identifying novel anticonvulsant agents indicated several widely-used artificial sweeteners as potential anticonvulsant candidates. Acesulfame potassium, cyclamate and saccharin were tested in the Maximal Electroshock Seizure model (mice, ip), showing moderate anticonvulsant activity. We hypothesized a probable structural link between the receptor responsible of sweet taste and anticonvulsant molecular targets. Bioinformatic tools confirmed a highly significant sequence-similarity between taste-related protein T1R3 and several metabotropic glutamate receptors from different species, including glutamate receptors upregulated in epileptogenesis and certain types of epilepsy. (C) 2012 Elsevier Ltd. All rights reserved.
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