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Chemical Kinetic Strategies for High‐Throughput Screening of Protein Aggregation Modulators
Author(s) -
Sárkány Zsuzsa,
Rocha Fernando,
Damas Ana M.,
MacedoRibeiro Sandra,
Martins Pedro M.
Publication year - 2019
Publication title -
chemistry – an asian journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.18
H-Index - 106
eISSN - 1861-471X
pISSN - 1861-4728
DOI - 10.1002/asia.201801703
Subject(s) - protein aggregation , amyloid (mycology) , high throughput screening , disease , chemistry , amyloid disease , computational biology , amyloid fibril , nanotechnology , biophysics , amyloid β , biology , biochemistry , medicine , materials science , inorganic chemistry
Insoluble aggregates staining positive to amyloid dyes are known histological hallmarks of different neurodegenerative disorders and of type II diabetes. Soluble oligomers are smaller assemblies whose formation prior to or concomitant with amyloid deposition has been associated to the processes of disease propagation and cell death. While the pathogenic mechanisms are complex and differ from disease to disease, both types of aggregates are important biological targets subject to intense investigation in academia and industry. Here we review recent advances in the fundamental understanding of protein aggregation that can be used on the development of anti‐amyloid and anti‐oligomerization drugs. Specifically, we pinpoint the chemical kinetic aspects that should be attended during the development of high‐throughput screening assays and in the hit validation phase. The strategies here devised are expected to establish a connection between basic research and pharmaceutical innovation.