% IMPORTANT: The following is UTF-8 encoded. This means that in the presence
% of non-ASCII characters, it will not work with BibTeX 0.99 or older.
% Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or
% “biber”.
@ARTICLE{Agerschou:888242,
author = {Agerschou, Emil Dandanell and Borgmann, Vera and
Wördehoff, Michael M. and Hoyer, Wolfgang},
title = {{I}nhibitor and substrate cooperate to inhibit amyloid
fibril elongation of α-synuclein},
journal = {Chemical science},
volume = {11},
number = {41},
issn = {2041-6539},
address = {Cambridge},
publisher = {RSC},
reportid = {FZJ-2020-04791},
pages = {11331 - 11337},
year = {2020},
abstract = {In amyloid fibril elongation, soluble growth substrate
binds to the fibril-end and converts into the fibril
conformation. This process is targeted by inhibitors that
block fibril-ends. Here, we investigated how the elongation
of α-synuclein (αS) fibrils, which are associated with
Parkinson's disease and other synucleinopathies, is
inhibited by αS variants with a preformed hairpin in the
critical N-terminal region comprising residues 36–57. The
inhibitory efficiency is strongly dependent on the specific
position of the hairpin. We find that the inhibitor and
substrate concentration dependencies can be analyzed with
models of competitive enzyme inhibition. Remarkably, the
growth substrate, i.e., wild-type αS, supports inhibition
by stabilizing the elongation-incompetent blocked state.
This observation allowed us to create inhibitor–substrate
fusions that achieved inhibition at low nanomolar
concentration. We conclude that inhibitor–substrate
cooperativity can be exploited for the design of fibril
growth inhibitors.},
cin = {IBI-7},
ddc = {540},
cid = {I:(DE-Juel1)IBI-7-20200312},
pnm = {553 - Physical Basis of Diseases (POF3-553) / BETACONTROL -
Control of amyloid formation via beta-hairpin molecular
recognition features (726368)},
pid = {G:(DE-HGF)POF3-553 / G:(EU-Grant)726368},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000582936200022},
doi = {10.1039/D0SC04051G},
url = {https://juser.fz-juelich.de/record/888242},
}