Crystal structures of human cholinesterases in complex with huprine W and tacrine: elements of specificity for anti-Alzheimer's drugs targeting acetyl- and butyryl-cholinesterase.

@article{Nachon2013CrystalSO,
  title={Crystal structures of human cholinesterases in complex with huprine W and tacrine: elements of specificity for anti-Alzheimer's drugs targeting acetyl- and butyryl-cholinesterase.},
  author={Florian Nachon and Eug{\'e}nie Carletti and Cyril Ronco and Marie Trovaslet and Yvain Nicolet and Ludovic Jean and Pierre-Yves Renard},
  journal={The Biochemical journal},
  year={2013},
  volume={453 3},
  pages={
          393-9
        }
}
The multifunctional nature of Alzheimer's disease calls for MTDLs (multitarget-directed ligands) to act on different components of the pathology, like the cholinergic dysfunction and amyloid aggregation. Such MTDLs are usually on the basis of cholinesterase inhibitors (e.g. tacrine or huprine) coupled with another active molecule aimed at a different target. To aid in the design of these MTDLs, we report the crystal structures of hAChE (human acetylcholinesterase) in complex with FAS-2… CONTINUE READING

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References

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SHOWING 1-10 OF 44 REFERENCES

Drosophila melanogaster acetylcholinesterase active site gorge by enlarging a back channel

Y. P. Pang, Y. Park, +3 authors K. Y. Zhu
  • FEBS J. 275,
  • 2012

XDS

  • Acta crystallographica. Section D, Biological crystallography
  • 2010

Features and development of Coot

  • Acta crystallographica. Section D, Biological crystallography
  • 2010