Publications by authors named "Anne Frycia"
A multi-disciplinary approach was used to identify the first pharmacophore model for KCC2 blockers: several physico-chemical studies such as XRD and NMR were combined to molecular modelling techniques, SAR analysis and synthesis of constrained analogues in order to determine a minimal conformational space regrouping few potential bioactive conformations. These conformations were further compared to the conformational space of a different series of KCC2 blockers in order to identify the common pharmacophoric features. The synthesis of more potent analogues in this second series confirmed the usefulness of this KCC2 blocker pharmacophore model.
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- Levetiracetam (Keppra) is a new medication approved for treating hard-to-control partial onset seizures in adults, showing good efficacy and tolerance due to its specific binding site in the brain.
- Researchers aimed to discover new drugs targeting the levetiracetam binding site (LBS) by modifying the structure of the original compound, finding that certain modifications improved the drug's potency against seizures.
- A promising drug candidate named ucb 34714 emerged from these modifications, showing to be ten times more effective than levetiracetam in mice and is set to enter phase II clinical trials.