The sulfonadyns: a class of aryl sulfonamides inhibiting dynamin I GTPase and clathrin mediated endocytosis are anti-seizure in animal models

Odell, Luke R.; Jones, Nigel C.; Chau, Ngoc; Robertson, Mark; Ambrus, Joseph I.; Deane, Fiona M.; Young, Kelly A.; Whiting, Ainslie; Xue, Jian; Prichard, Kate L.; Daniel, James; Gorgani, Nick N.; O'brien, Terence J; Robinson, Phillip J.; McCluskey, Adam

doi:10.1039/d2md00371f

RSC Med. Chem.

2023

DOI: 10.1039/d2md00371f

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The sulfonadyns: a class of aryl sulfonamides inhibiting dynamin I GTPase and clathrin mediated endocytosis are anti-seizure in animal models

Luke R. Odell

Nigel C. Jones

Ngoc Chau

et al.

Abstract: We show that dansylcadaverine (1) a known in-cell inhibitor of clathrin mediated endocytosis (CME), moderately inhibits dynamin I (dynI) GTPase activity (IC50 45 μM) and transferrin (Tfn) endocytosis in U2OS...

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2024

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Presynaptic antiseizure medications - basic mechanisms and clues for their rational combinations

Czapińska-Ciepiela,

Łuszczki,

Czapiński

et al. 2024

Pharmacol. Rep

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Among clinically highly efficient antiseizure medications (ASMs) there are modifiers of the presynaptic release machinery. Of them, levetiracetam and brivaracetam show a high affinity to the synaptic vesicle protein type 2 A (SV2A), whereas pregabalin and gabapentin are selective ligands for the α2δ1 subunits of the voltage-gated calcium channels. In this paper, we present recent progress in understanding the significance of presynaptic release machinery in the neurochemical mechanisms of epilepsy and ASMs. Furthermore, we discuss whether the knowledge of the basic mechanisms of the presynaptically acting ASMs might help establish a rational polytherapy for drug-resistant epilepsy.

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Presynaptic antiseizure medications - basic mechanisms and clues for their rational combinations

Czapińska-Ciepiela,

Łuszczki,

Czapiński

et al. 2024

Pharmacol. Rep

View full text Add to dashboard Cite

show abstract

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The sulfonadyns: a class of aryl sulfonamides inhibiting dynamin I GTPase and clathrin mediated endocytosis are anti-seizure in animal models

Abstract: We show that dansylcadaverine (1) a known in-cell inhibitor of clathrin mediated endocytosis (CME), moderately inhibits dynamin I (dynI) GTPase activity (IC50 45 μM) and transferrin (Tfn) endocytosis in U2OS...

Cited by 1 publication

References 85 publications

Presynaptic antiseizure medications - basic mechanisms and clues for their rational combinations

Presynaptic antiseizure medications - basic mechanisms and clues for their rational combinations

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