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@ARTICLE{Eberle:908872,
author = {Eberle, Raphael J. and Gering, Ian and Tusche, Markus and
Ostermann, Philipp N. and Müller, Lisa and Adams, Ortwin
and Schaal, Heiner and Olivier, Danilo S. and Amaral, Marcos
S. and Arni, Raghuvir K. and Willbold, Dieter and Coronado,
Mônika A.},
title = {{D}esign of {D}-{A}mino {A}cids {SARS}-{C}o{V}-2 {M}ain
{P}rotease {I}nhibitors {U}sing the {C}ationic {P}eptide
from {R}attlesnake {V}enom as a {S}caffold},
journal = {Pharmaceuticals},
volume = {15},
number = {5},
issn = {1424-8247},
address = {Basel},
publisher = {MDPI},
reportid = {FZJ-2022-02886},
pages = {540 -},
year = {2022},
abstract = {The C30 endopeptidase (3C-like protease; 3CLpro) is
essential for the life cycle of SARS-CoV-2 (severe acute
respiratory syndrome-coronavirus-2) since it plays a pivotal
role in viral replication and transcription and, hence, is a
promising drug target. Molecules isolated from animals,
insects, plants, or microorganisms can serve as a scaffold
for the design of novel biopharmaceutical products.
Crotamine, a small cationic peptide from the venom of the
rattlesnake Crotalus durissus terrificus, has been the focus
of many studies since it exhibits activities such as
analgesic, in vitro antibacterial, and hemolytic activities.
The crotamine derivative L-peptides (L-CDP) that inhibit the
3CL protease in the low µM range were examined since they
are susceptible to proteolytic degradation; we explored the
utility of their D-enantiomers form. Comparative uptake
inhibition analysis showed D-CDP as a promising prototype
for a D-peptide-based drug. We also found that the
D-peptides can impair SARS-CoV-2 replication in vivo,
probably targeting the viral protease 3CLpro.},
cin = {IBI-7},
ddc = {610},
cid = {I:(DE-Juel1)IBI-7-20200312},
pnm = {5244 - Information Processing in Neuronal Networks
(POF4-524)},
pid = {G:(DE-HGF)POF4-5244},
typ = {PUB:(DE-HGF)16},
pubmed = {35631367},
UT = {WOS:000803447200001},
doi = {10.3390/ph15050540},
url = {https://juser.fz-juelich.de/record/908872},
}