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- W2034653510 abstract "Targeting of the microtubule-associated protein tau that pathologically accumulates in Alzheimer's disease (AD) has emerged as the effective strategy for treating AD. Tau normally functions to stabilize microtubules in neurons, but pathologically aggregates in AD and other tauopathies, forming neurofibrillary tangles characterized as intracellular aggregates composed of paired helical filaments containing tau protein. ProteoTech Inc. has developed a number of different in vitro screening technologies, and cellular and animal models that allow for the identification of new and potent inhibitors of amyloidosis in general. Exebryl-1® and other novel small molecules were found to be potent inhibitors of tau aggregates. Novel small molecules developed at ProteoTech [including Exebryl-1® previously found to be a potent inhibitor of beta-amyloid (Abeta) protein aggregation] were screened for their ability to inhibit/disrupt tau fibril formation using in vitro Thioflavin T fluorometry. Select small molecules were further tested for their ability to affect intracellular tau multimerization and aggregation in newly developed cell models that express tau repeat domains by western analysis for soluble and insoluble tau aggregates, and by florescent staining for aggregated tau. A number of the ProteoTech novel small molecules caused a dose-dependent disruption of preformed tau aggregates (IC50 range from 1.60 μM to 66 μM) in ThioT assays. Using a sensitive western analysis that could quantitatively determine levels of monomers and oligomers/aggregates of tau in soluble and insoluble components of tau-expressing cell lysates, we confirmed that phenothiazine methylene blue (i.e. positive control) markedly affected tau aggregation in our cellular models. In preliminary experiments, we found that Exebryl-1® and other small molecule compounds identified as potent tau aggregation inhibitors in vitro also reduced levels of insoluble tau oligomers in cell culture. Exebryl-1® is a novel small molecule that appears to inhibit both Abeta and tau protein aggregation thus suggesting that it may be the first drug to be developed for AD, able to reduce both amyloid plaque and neurofibrillary tangle accumulation." @default.
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- W2034653510 date "2011-07-01" @default.
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- W2034653510 title "P2‐529: Identification of Exebryl‐1® and other novel small molecules as tau protein aggregation inhibitors" @default.
- W2034653510 doi "https://doi.org/10.1016/j.jalz.2011.05.1398" @default.
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