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Structures of Human Acetylcholinesterase in Complex with Pharmacologically Important Ligands
Abstract
Human acetylcholinesterase (AChE) is a significant target for therapeutic drugs. Here we present high resolution crystal structures of human AChE, alone and in complexes with drug ligands; donepezil, an Alzheimer's disease drug, binds differently to human AChE than it does to Torpedo AChE. These crystals of human AChE provide a more accurate platform for further drug development than previously available.
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Cited by
Outcomes of Alzheimer's disease therapy with acetylcholinesterase inhibitors and memantine
Zemek, F., Drtinova, L., Nepovimova, E., Sepsova, V., Korabecny, J., Klimes, J., & Kuca, K. (2014) · Expert Opinion on Drug Safety · doi:10.1517/14740338.2014.914168 · Cited by 299
Rochais, C., Lecoutey, C., Gaven, F., Giannoni, P., Hamidouche, K., Hedou, D., Dubost, E., Genest, D., Yahiaoui, S., Freret, T., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00115 · Cited by 129
El-Hawary, S. S., Sobeh, M., Badr, W. K., Abdelfattah, M. A. O., Ali, Z. Y., El-Tantawy, M. E., Rabeh, M. A., & Wink, M. (2020) · Saudi Journal of Biological Sciences · doi:10.1016/j.sjbs.2020.07.003 · Cited by 102
Hoffmann, M., Stiller, C., Endres, E., Scheiner, M., Gunesch, S., Sotriffer, C., Maurice, T., & Decker, M. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01012 · Cited by 105
Dhamodharan, G., & Mohan, C. G. (2022) · Molecular Diversity · doi:10.1007/s11030-021-10282-8 · Cited by 56
Metadata
- Authors
- Cheung, J., Rudolph, M. J., Burshteyn, F., Cassidy, M. S., Gary, E. N., Love, J., Franklin, M. C., & Height, J. J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2012-11-12
- Volume
- 55
- Issue
- 22
- Pages
- 10282-10286
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2112006614
- Cited by
- 1,356
- References
- 0
- FWCI
- 14.87
- Type
- journal article
- Language
- en
- Open access
- closed
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- The paper
- Cheung, J., Rudolph, M. J., Burshteyn, F., Cassidy, M. S., Gary, E. N., Love, J., Franklin, M. C., & Height, J. J. (2012). Structures of Human Acetylcholinesterase in Complex with Pharmacologically Important Ligands. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm300871x
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
