scholarly journals Discovery of small molecule inhibitors against the NS3/4A serine protease of Hepatitis C virus genotype 3 via highthroughput virtual screening and in vitro evaluations

2020 ◽  
Vol 37 (3) ◽  
pp. 609-625
2019 ◽  
Vol 24 (37) ◽  
pp. 4484-4491 ◽  
Author(s):  
Sara M. El-Sayed ◽  
Mohamed A.M. Ali ◽  
Bahaa El-Dien M. El- Gendy ◽  
Samar S. Dandash ◽  
Yvette Issac ◽  
...  

2019 ◽  
Vol 26 (4) ◽  
pp. 459-465 ◽  
Author(s):  
Sang Soo Lee ◽  
Cha Young Kim ◽  
Bo Ra Kim ◽  
Ra Ri Cha ◽  
Wan Soo Kim ◽  
...  

2003 ◽  
Vol 77 (6) ◽  
pp. 3669-3679 ◽  
Author(s):  
Caterina Trozzi ◽  
Linda Bartholomew ◽  
Alessandra Ceccacci ◽  
Gabriella Biasiol ◽  
Laura Pacini ◽  
...  

ABSTRACT The hepatitis C virus (HCV) serine protease is necessary for viral replication and represents a valid target for developing new therapies for HCV infection. Potent and selective inhibitors of this enzyme have been identified and shown to inhibit HCV replication in tissue culture. The optimization of these inhibitors for clinical development would greatly benefit from in vitro systems for the identification and the study of resistant variants. We report the use HCV subgenomic replicons to isolate and characterize mutants resistant to a protease inhibitor. Taking advantage of the replicons' ability to transduce resistance to neomycin, we selected replicons with decreased sensitivity to the inhibitor by culturing the host cells in the presence of the inhibitor and neomycin. The selected replicons replicated to the same extent as those in parental cells. Sequence analysis followed by transfection of replicons containing isolated mutations revealed that resistance was mediated by amino acid substitutions in the protease. These results were confirmed by in vitro experiments with mutant enzymes and by modeling the inhibitor in the three-dimensional structure of the protease.


2010 ◽  
Vol 82 (10) ◽  
pp. 1647-1654 ◽  
Author(s):  
Christine Larsen ◽  
Vanina Bousquet ◽  
Elisabeth Delarocque-Astagneau ◽  
Corinne Pioche ◽  
Françoise Roudot-Thoraval

2013 ◽  
Vol 13 (8) ◽  
Author(s):  
Faraz Salehi Moghadam ◽  
Seyed Reza Mohebbi ◽  
Seyed Masoud Hosseini ◽  
Behzad Damavand ◽  
Mohammad Reza Zali

2008 ◽  
Vol 16 (4) ◽  
pp. 1874-1883 ◽  
Author(s):  
Kevin X. Chen ◽  
Bancha Vibulbhan ◽  
Weiying Yang ◽  
Kuo-Chi Cheng ◽  
Rong Liu ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document