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[Design of acetylcholinesterase inhibitor for Alzheimer's disease therapy: from multi-binding site inhibitors to multi-target directed ligands].
Yao Xue Xue Bao. 2012 Mar; 47(3):313-21.YX

Abstract

Alzheimer's disease (AD) is a complex neurodegenerative disorder which seriously causes the dementia in elderly people and afflicts millions of people worldwide. Drug discovery for Alzheimer's disease therapy has been a hot research area and a big challenge, in which development of acetylcholinesterase (AChE) inhibitors design was the most active and some AChE inhibitors are commercially available for AD medication already. However, practical using of commercial AChE inhibitors showed their limited usefulness and related adverse effects. Thus, it is extremely urgent to find novel AChE inhibitors with higher potency and less adverse effects. Based on the accurate crystallographic studies about AChE, strategies for multi-binding site AChE inhibitors have been formed, followed by design of the multi-target directed ligands. In this review, the structures and binding modes of commercial AChE inhibitors were briefly discussed, together with the development of AChE inhibitor design for AD therapy: from multi-binding site inhibitors to multi-target directed ligands.

Authors+Show Affiliations

Yang WC
Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, China.
Sun Q
No affiliation info available
Yu NX
No affiliation info available
Zhu XL
No affiliation info available
Yang GF
No affiliation info available

MeSH

AcetylcholinesteraseAlzheimer DiseaseAmyloid Precursor Protein SecretasesAmyloid beta-PeptidesAnimalsAspartic Acid EndopeptidasesBinding SitesButyrylcholinesteraseCholinesterase InhibitorsDrug DesignHumansLigandsMonoamine Oxidase InhibitorsReceptors, N-Methyl-D-AspartateStructure-Activity Relationship

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

chi

PubMed ID

22645754

Citation

Yang, Wen-Chao, et al. "[Design of Acetylcholinesterase Inhibitor for Alzheimer's Disease Therapy: From Multi-binding Site Inhibitors to Multi-target Directed Ligands]." Yao Xue Xue Bao = Acta Pharmaceutica Sinica, vol. 47, no. 3, 2012, pp. 313-21.
Yang WC, Sun Q, Yu NX, et al. [Design of acetylcholinesterase inhibitor for Alzheimer's disease therapy: from multi-binding site inhibitors to multi-target directed ligands]. Yao Xue Xue Bao. 2012;47(3):313-21.
Yang, W. C., Sun, Q., Yu, N. X., Zhu, X. L., & Yang, G. F. (2012). [Design of acetylcholinesterase inhibitor for Alzheimer's disease therapy: from multi-binding site inhibitors to multi-target directed ligands]. Yao Xue Xue Bao = Acta Pharmaceutica Sinica, 47(3), 313-21.
Yang WC, et al. [Design of Acetylcholinesterase Inhibitor for Alzheimer's Disease Therapy: From Multi-binding Site Inhibitors to Multi-target Directed Ligands]. Yao Xue Xue Bao. 2012;47(3):313-21. PubMed PMID: 22645754.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Design of acetylcholinesterase inhibitor for Alzheimer's disease therapy: from multi-binding site inhibitors to multi-target directed ligands]. AU - Yang,Wen-Chao, AU - Sun,Qi, AU - Yu,Ning-Xi, AU - Zhu,Xiao-Lei, AU - Yang,Guang-Fu, PY - 2012/5/31/entrez PY - 2012/5/31/pubmed PY - 2013/8/13/medline SP - 313 EP - 21 JF - Yao xue xue bao = Acta pharmaceutica Sinica JO - Yao Xue Xue Bao VL - 47 IS - 3 N2 - Alzheimer's disease (AD) is a complex neurodegenerative disorder which seriously causes the dementia in elderly people and afflicts millions of people worldwide. Drug discovery for Alzheimer's disease therapy has been a hot research area and a big challenge, in which development of acetylcholinesterase (AChE) inhibitors design was the most active and some AChE inhibitors are commercially available for AD medication already. However, practical using of commercial AChE inhibitors showed their limited usefulness and related adverse effects. Thus, it is extremely urgent to find novel AChE inhibitors with higher potency and less adverse effects. Based on the accurate crystallographic studies about AChE, strategies for multi-binding site AChE inhibitors have been formed, followed by design of the multi-target directed ligands. In this review, the structures and binding modes of commercial AChE inhibitors were briefly discussed, together with the development of AChE inhibitor design for AD therapy: from multi-binding site inhibitors to multi-target directed ligands. SN - 0513-4870 UR - https://www.unboundmedicine.com/medline/citation/22645754/[Design_of_acetylcholinesterase_inhibitor_for_Alzheimer's_disease_therapy:_from_multi_binding_site_inhibitors_to_multi_target_directed_ligands]_ L2 - https://medlineplus.gov/alzheimersdisease.html DB - PRIME DP - Unbound Medicine ER -

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