Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).

@article{Bartolucci2006StructuralDO,
  title={Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).},
  author={Cecilia Bartolucci and Mariacristina Siotto and Eleonora Ghidini and Gabriele Amari and Pier Tonino Bolzoni and Marco Racchi and Gino Villetti and Maurizio Delcanale and Doriano Lamba},
  journal={Journal of medicinal chemistry},
  year={2006},
  volume={49 17},
  pages={5051-8}
}
Ganstigmine is an orally active, geneserine derived, carbamate-based acetylcholinesterase inhibitor developed for the treatment of Alzheimer's disease. The crystal structure of the ganstigmine conjugate with Torpedo californica acetylcholinesterase (TcAChE) has been determined at 2.40 A resolution, and a detailed structure-based analysis of the in vitro and ex vivo anti-AChE activity by ganstigmine and by new geneserine derivatives is presented. The carbamoyl moiety is covalently bound to the… CONTINUE READING

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