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Repositioning tolcapone as a potent inhibitor of transthyretin amyloidogenesis ...

Sant'Anna, R; Gallego, P; Robinson, L; Pereira-Henriques, A; Ferreira, N; Pinheiro, F; Esperante, S; Pallares, I; Huertas, O; Almeida, M; Reixach, N

Transthyretin (TTR) is a plasma homotetrameric protein implicated in fatal systemic amyloidoses. TTR tetramer dissociation precedes pathological TTR aggregation. Native state stabilizers are promising drugs to treat TTR amyloidoses. Here we repurpose tolcapone, an FDA-approved molecule for Parkinson's disease, as a potent TTR aggregation inhibitor. Tolcapone binds specifically to TTR in human plasma, stabilizes...

Date: 2016   |   Origin: Repositório Aberto da Universidade do Porto
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