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Cataldi, R.

Publications and source records attributed to Cataldi, R..

2 recordsLinked to original sources

In situ generation of Aβ42 oligomers via secondary nucleation triggers neurite degeneration and synaptic dysfunction in human iPSC-derived glutamatergic neurons

The aggregation of A{beta}42 into misfolded oligomers is a central event in the pathogenesis of Alzheimers disease. In this study, we aimed to develop a robust experimental system that recapitulates A{beta}42 oligomerization in living cells to gain insight into their neurotoxicity and to provide a platform to characterize the effects of inhibitors of this process. Our strategy is based on the in situ generation of A{beta}42 oligomers via secondary nucleation by repeatedly treating the cells with A{beta}42 monomers in the presence of pre-formed A{beta}42 fibrils. This approach enables an accurate control over the levels of on-pathway soluble A{beta}42 oligomers and cell-associated aggregates, as well as the study of their neurotoxic effects. By implementing this approach in human glutamatergic neurons derived from induced pluripotent stem cells (iPSCs), we were able to replicate key aspects of Alzheimers disease, including neurite degeneration and synaptic dysfunction. Using BRICHOS, a molecular chaperone that specifically inhibits secondary nucleation, we confirmed that aggregation in this system occurs through secondary nucleation, and that quantitative parameters for comparing potential A{beta}42 aggregation inhibitors can be obtained. Overall, our results demonstrate that by in situ generation of on-pathway A{beta}42 oligomers, one can obtain translational cellular models of AD to bridge the gap between basic research and clinical applications.

cell biology↗

Structure-based discovery of small molecule inhibitors of the autocatalytic proliferation of alpha-synuclein aggregates

The presence of amyloid fibrils of -synuclein is closely associated with Parkinsons disease and related synucleinopathies. It is still very challenging, however, to systematically discover small molecules that prevent the formation of these aberrant aggregates. Here, we describe a structure-based approach to identify small molecules that specifically inhibit the surface-catalyzed secondary nucleation step in the aggregation of -synuclein by binding to the surface of the amyloid fibrils. The resulting small molecules are screened using a combination of kinetic and thermodynamic assays for their ability to bind -synuclein fibrils and prevent the further generation of toxic oligomers. This study demonstrates that the combination of structure-based and kinetic-based drug discovery methods can lead to the identification of small molecules that selectively inhibit the autocatalytic proliferation of -synuclein aggregates.

biophysics↗