Blockade of enzyme activity inhibits tissue transglutaminase-mediated transamidation of α-synuclein in a cellular model of Parkinson's disease.

@article{Verhaar2011BlockadeOE,
  title={Blockade of enzyme activity inhibits tissue transglutaminase-mediated transamidation of α-synuclein in a cellular model of Parkinson's disease.},
  author={Robin Verhaar and Cornelis A. M. Jongenelen and Melanie G{\'e}rard and Veerle Baekelandt and Anne-Marie van Dam and Micha M. M. Wilhelmus and Benjamin Drukarch},
  journal={Neurochemistry international},
  year={2011},
  volume={58 7},
  pages={785-93}
}
Transamidation of α-synuclein by the Ca(2+)-dependent enzyme tissue transglutaminase (tTG, EC 2.3.2.13) is implicated in Parkinson's disease (PD). tTG may therefore offer a novel therapeutic target to intervene in PD. Here we first evaluated the potency and efficacy of three recently developed irreversible active-site inhibitors of tTG (B003, Z006 and KCC009) to inhibit tTG activity in vitro and in living cells. In vitro, all compounds were found to be full inhibitors of tTG activity showing a… CONTINUE READING

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