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Development of tau aggregation inhibitors for Alzheimer's disease.
Angew Chem Int Ed Engl. 2009; 48(10):1740-52.AC

Abstract

A variety of human diseases are suspected to be directly linked to protein misfolding. Highly organized protein aggregates, called amyloid fibrils, and aggregation intermediates are observed; these are considered to be mediators of cellular toxicity and thus attract a great deal of attention from investigators. Neurodegenerative pathologies such as Alzheimer's disease account for a major part of these protein misfolding diseases. The last decade has witnessed a renaissance of interest in inhibitors of tau aggregation as potential disease-modifying drugs for Alzheimer's disease and other "tauopathies". The recent report of a phase II clinical trial with the tau aggregation inhibitor MTC could hold promise for the validation of the concept. This Review summarizes the available data concerning small-molecule inhibitors of tau aggregation from a medicinal chemistry point of view.

Links

Publisher Full Text (DOI)

Authors+Show Affiliations

Bulic B
Max-Planck-Institute for Molecular Physiology, Dortmund, Germany. bruno.bulic@mpi-dortmund.mpg.de
Pickhardt M
No affiliation info available
Schmidt B
No affiliation info available
Mandelkow EM
No affiliation info available
Waldmann H
No affiliation info available
Mandelkow E
No affiliation info available

MeSH

Alzheimer DiseaseAmyloidAmyloid beta-PeptidesBenzothiazolesDatabases, FactualHumansTauopathiesThiazolestau Proteins

Pub Type(s)

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

Language

eng

PubMed ID

19189357

Citation

Bulic, Bruno, et al. "Development of Tau Aggregation Inhibitors for Alzheimer's Disease." Angewandte Chemie (International Ed. in English), vol. 48, no. 10, 2009, pp. 1740-52.
Bulic B, Pickhardt M, Schmidt B, et al. Development of tau aggregation inhibitors for Alzheimer's disease. Angew Chem Int Ed Engl. 2009;48(10):1740-52.
Bulic, B., Pickhardt, M., Schmidt, B., Mandelkow, E. M., Waldmann, H., & Mandelkow, E. (2009). Development of tau aggregation inhibitors for Alzheimer's disease. Angewandte Chemie (International Ed. in English), 48(10), 1740-52. https://doi.org/10.1002/anie.200802621
Bulic B, et al. Development of Tau Aggregation Inhibitors for Alzheimer's Disease. Angew Chem Int Ed Engl. 2009;48(10):1740-52. PubMed PMID: 19189357.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of tau aggregation inhibitors for Alzheimer's disease. AU - Bulic,Bruno, AU - Pickhardt,Marcus, AU - Schmidt,Boris, AU - Mandelkow,Eva-Maria, AU - Waldmann,Herbert, AU - Mandelkow,Eckhard, PY - 2009/2/4/entrez PY - 2009/2/4/pubmed PY - 2009/4/3/medline SP - 1740 EP - 52 JF - Angewandte Chemie (International ed. in English) JO - Angew Chem Int Ed Engl VL - 48 IS - 10 N2 - A variety of human diseases are suspected to be directly linked to protein misfolding. Highly organized protein aggregates, called amyloid fibrils, and aggregation intermediates are observed; these are considered to be mediators of cellular toxicity and thus attract a great deal of attention from investigators. Neurodegenerative pathologies such as Alzheimer's disease account for a major part of these protein misfolding diseases. The last decade has witnessed a renaissance of interest in inhibitors of tau aggregation as potential disease-modifying drugs for Alzheimer's disease and other "tauopathies". The recent report of a phase II clinical trial with the tau aggregation inhibitor MTC could hold promise for the validation of the concept. This Review summarizes the available data concerning small-molecule inhibitors of tau aggregation from a medicinal chemistry point of view. SN - 1521-3773 UR - https://www.unboundmedicine.com/medline/citation/19189357/Development_of_tau_aggregation_inhibitors_for_Alzheimer's_disease_ L2 - https://doi.org/10.1002/anie.200802621 DB - PRIME DP - Unbound Medicine ER -