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A Potent Sybody Selectively Inhibits α-Synuclein Amyloid Formation by Binding to the P1 Region.

Authors :
Gialama D
Vadukul DM
Thrush RJ
Radford SE
Aprile FA
Source :
Journal of medicinal chemistry [J Med Chem] 2024 Jun 27; Vol. 67 (12), pp. 9857-9868. Date of Electronic Publication: 2024 Jun 06.
Publication Year :
2024

Abstract

Increasing research efforts focus on exploiting antibodies to inhibit the amyloid formation of neurodegenerative proteins. Nevertheless, it is challenging to discover antibodies that inhibit this process in a specific manner. Using ribosome display, we screened for synthetic single-domain antibodies, i.e., sybodies, of the P1 region of α-synuclein (residues 36-42), a protein that forms amyloid in Parkinson's disease and multiple-system atrophy. Hits were assessed for direct binding to a P1 peptide and the inhibition of amyloid formation. We discovered a sybody, named αSP1, that inhibits amyloid formation of α-synuclein at substoichiometric concentrations in a specific manner, even within highly crowded heterogeneous mixtures. Fluorescence resonance energy transfer-based binding assays and seeding experiments with and without αSP1 further demonstrate the importance of the P1 region for both primary and secondary nucleation mechanisms of amyloid assembly.

Details

Language :
English
ISSN :
1520-4804
Volume :
67
Issue :
12
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
38842931
Full Text :
https://doi.org/10.1021/acs.jmedchem.3c02408