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@ARTICLE{Oerlemans:576716,
author = {Oerlemans, Rick and Ruiz-Moreno, Angel Jonathan and Cong,
Yingying and Dinesh Kumar, Nilima and Velasco-Velazquez,
Marco A and Neochoritis, Constantinos G and Smith, Jolanda
and Reggiori, Fulvio and Groves, Matthew R and Dömling,
Alexander},
title = {{R}epurposing the {HCV} {NS}3-4{A} protease drug boceprevir
as {COVID}-19 therapeutics.},
journal = {RSC medicinal chemistry},
volume = {12},
number = {3},
issn = {2040-2503},
address = {Cambridge},
publisher = {Royal Society of Chemistry},
reportid = {PUBDB-2023-00887},
pages = {370 - 379},
year = {2020},
note = {ISSN 2632-8682 not unique: **2 hits**.},
abstract = {The rapid growth of COVID-19 cases is causing an increasing
death toll and also paralyzing the world economy. De novo
drug discovery takes years to move from idea and/or
pre-clinic to market, and it is not a short-term solution
for the current SARS-CoV-2 pandemic. Drug repurposing is
perhaps the only short-term solution, while vaccination is a
middle-term solution. Here, we describe the discovery path
of the HCV NS3-4A protease inhibitors boceprevir and
telaprevir as SARS-CoV-2 main protease (3CLpro) inhibitors.
Based on our hypothesis that α-ketoamide drugs can
covalently bind to the active site cysteine of the
SARS-CoV-2 3CLpro, we performed docking studies, enzyme
inhibition and co-crystal structure analyses and finally
established that boceprevir, but not telaprevir, inhibits
replication of SARS-CoV-2 and mouse hepatitis virus (MHV),
another coronavirus, in cell culture. Based on our studies,
the HCV drug boceprevir deserves further attention as a
repurposed drug for COVID-19 and potentially other
coronaviral infections as well.},
cin = {DOOR ; HAS-User},
ddc = {540},
cid = {I:(DE-H253)HAS-User-20120731},
pnm = {6G3 - PETRA III (DESY) (POF4-6G3)},
pid = {G:(DE-HGF)POF4-6G3},
experiment = {EXP:(DE-H253)P-P11-20150101},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:34041486},
pmc = {pmc:PMC8130630},
UT = {WOS:000635760100004},
doi = {10.1039/D0MD00367K},
url = {https://bib-pubdb1.desy.de/record/576716},
}