scholarly journals Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-Throughput Screening

2020 ◽  
Vol 3 (5) ◽  
pp. 1008-1016
Author(s):  
Wei Zhu ◽  
Miao Xu ◽  
Catherine Z. Chen ◽  
Hui Guo ◽  
Min Shen ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
High Throughput ◽  
High Throughput Screening ◽  
3Cl Protease

scholarly journals Application of Acoustic Ejection MS System to High-Throughput Screening for SARS-CoV-2 3CL Protease Inhibitors

2021 ◽  
Author(s):  
Tsukasa Hasegawa ◽  
Riyo M. Imamura ◽  
Tateki Suzuki ◽  
Takao Hashiguchi ◽  
Takao Nomura ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
High Throughput ◽  
High Throughput Screening ◽  
3Cl Protease

scholarly journals In Silico Prediction of SARS Protease Inhibitors by Virtual High Throughput Screening

2007 ◽  
Vol 69 (4) ◽  
pp. 269-279 ◽  
Author(s):  
Dariusz Plewczynski ◽  
Marcin Hoffmann ◽  
Marcin von Grotthuss ◽  
Krzysztof Ginalski ◽  
Leszek Rychewski
Keyword(s):  
Protease Inhibitors ◽  
High Throughput ◽  
In Silico ◽  
High Throughput Screening ◽  
In Silico Prediction

A novel high throughput screening assay for HCV NS3 serine protease inhibitors

2003 ◽  
Vol 107 (2) ◽  
pp. 245-255 ◽  
Author(s):  
Yevgeny Berdichevsky ◽  
Romy Zemel ◽  
Larisa Bachmatov ◽  
Alex Abramovich ◽  
Ruth Koren ◽  
...  
Keyword(s):  
Serine Protease ◽  
Protease Inhibitors ◽  
High Throughput ◽  
High Throughput Screening ◽  
Serine Protease Inhibitors ◽  
Screening Assay ◽  
High Throughput Screening Assay

scholarly journals Discovery of SARS-CoV-2 Papain-like Protease Inhibitors through a Combination of High-Throughput Screening and a FlipGFP-Based Reporter Assay

2021 ◽  
Author(s):  
Chunlong Ma ◽  
Michael Dominic Sacco ◽  
Zilei Xia ◽  
George Lambrinidis ◽  
Julia Alma Townsend ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
High Throughput ◽  
High Throughput Screening ◽  
Reporter Assay

scholarly journals Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening

2020 ◽  
Author(s):  
Wei Zhu ◽  
Miao Xu ◽  
Catherine Z. Chen ◽  
Hui Guo ◽  
Min Shen ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Drug Target ◽  
Cytopathic Effect ◽  
Drug Repurposing ◽  
Combination Therapies ◽  
Main Protease ◽  
Investigational Drugs ◽  
3Cl Protease ◽  
Viral Enzyme

AbstractThe outbreak of coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has emphasized the urgency to develop effective therapeutics. Drug repurposing screening is regarded as one of the most practical and rapid approaches for the discovery of such therapeutics. The 3C like protease (3CLpro), or main protease (Mpro) of SARS-CoV-2 is a valid drug target as it is a specific viral enzyme and plays an essential role in viral replication. We performed a quantitative high throughput screening (qHTS) of 10,755 compounds consisting of approved and investigational drugs, and bioactive compounds using a SARS-CoV-2 3CLpro assay. Twenty-three small molecule inhibitors of SARS-CoV-2 3CLpro have been identified with IC50s ranging from 0.26 to 28.85 μM. Walrycin B (IC50 = 0.26 µM), Hydroxocobalamin (IC50 = 3.29 µM), Suramin sodium (IC50 = 6.5 µM), Z-DEVD-FMK (IC50 = 6.81 µM), LLL-12 (IC50 = 9.84 µM), and Z-FA-FMK (IC50 = 11.39 µM) are the most potent 3CLpro inhibitors. The activities of anti-SARS-CoV-2 viral infection was confirmed in 7 of 23 compounds using a SARS-CoV-2 cytopathic effect assay. The results demonstrated a set of SARS-CoV-2 3CLpro inhibitors that may have potential for further clinical evaluation as part of drug combination therapies to treating COVID-19 patients, and as starting points for chemistry optimization for new drug development.

High-throughput screening program for botanical extracts

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
L Hingorani ◽  
NP Seeram ◽  
B Ebersole
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Screening Program ◽  
Botanical Extracts

High throughput screening of microbial biodiversity for the discovery of novel cosmeceutical agents

Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
K Georgousaki ◽  
N DePedro ◽  
AM Chinchilla ◽  
N Aliagiannis ◽  
F Vicente ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Microbial Biodiversity

High throughput screening to investigate Brazilian Cerrado biome plant extract bank chemical diversity

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
LS Espindola ◽  
RG Dusi ◽  
KR Gustafson ◽  
J McMahon ◽  
JA Beutler
Keyword(s):  
High Throughput ◽  
Plant Extract ◽  
High Throughput Screening ◽  
Chemical Diversity ◽  
Brazilian Cerrado ◽  
Cerrado Biome

High-throughput screening revealed a clinically relevant drug to induce sperm motility

2014 ◽  
Author(s):  
Clair Cochrane ◽  
Halil Ruso ◽  
Anthony Hope ◽  
Rosemary G Clarke ◽  
Christopher Barratt ◽  
...  
Keyword(s):  
Sperm Motility ◽  
High Throughput ◽  
High Throughput Screening
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