scholarly journals Repurposing the HCV NS3–4A protease drug boceprevir as COVID-19 therapeutics

2021 ◽  
Author(s):  
Rick Oerlemans ◽  
Angel Jonathan Ruiz-Moreno ◽  
Yingying Cong ◽  
Nilima Dinesh Kumar ◽  
Marco A. Velasco-Velazquez ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Hcv Protease ◽  
Viral Proliferation

α-Ketoamide HCV protease inhibitors covalently bind to SARS-CoV-2 3CLpro. Boceprevir is a particular promising repurposed drug as it potently inhibits cellular viral proliferation.

HCV protease inhibitors bring new options for patients

2011 ◽  
Vol 68 (15) ◽  
pp. 1372-1379
Author(s):  
Kate Traynor
Keyword(s):  
Protease Inhibitors ◽  
Hcv Protease

scholarly journals Naturally occurring mutations to HCV protease inhibitors in treatment-naïve patients

2012 ◽  
Vol 9 (1) ◽  
pp. 245 ◽  
Author(s):  
Stefania Paolucci ◽  
Loretta Fiorina ◽  
Antonio Piralla ◽  
Roberto Gulminetti ◽  
Stefano Novati ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Naturally Occurring ◽  
Treatment Naïve ◽  
Hcv Protease

Determination of binding potential of HCV protease inhibitors against SARS-CoV-2 Papain-like protease with computational docking

2021 ◽  
Vol 18 ◽  
Author(s):  
Zihni Onur Çalışkaner
Keyword(s):  
Protease Inhibitors ◽  
Drug Repurposing ◽  
Docking Study ◽  
Binding Energies ◽  
Binding Potential ◽  
Computational Docking ◽  
In Silico Docking ◽  
Hcv Protease ◽  
Novel Coronavirus ◽  
Inhibitory Molecules

Background: SARS-CoV-2, a novel coronavirus that causes a pandemic respiratory disease, has recently emerged from China. Since it’s a life-threatening virus, investigation of curative medications along with protective vaccines still maintains its importance. Drug repurposing is a reasonable and immediate approach to combat SARS-CoV-2 infection by identifying inhibitory molecules from marketed drugs. PL protease (PLpro.) is one of the essential enzymes for the progression of SARS-CoV-2 replication and life cycle. Objective: We aimed to investigate the potential of 4 HCV protease inhibitors as probable repurposing drugs in Covid-19 treatment. Methods: In order to understand the possible binding affinity of HCV protease inhibitors, Boceprevir, Grazoprevir, Simeprevir, and Telaprevir, against to PLpro, we performed docking analysis in silico. Docking study was accomplished using AutoDock 4.2 software. Potential druggable pockets on PLpro were predicted by DoGSiteScorer tool in order to explore any overlapping with binding regions and these pockets. Results: This analysis demonstrated Boceprevir, Grazoprevir, Simeprevir and Telaprevir interacted by PLpro with binding energies (kcal/mol) of -4.97, -4.24, -6.98, -1.08, respectively. Asn109, one of the interacted residues with both Boceprevir and Simeprevir, is a neighbouring residue to catalytic Cys111. Additionally, Telaprevir notably interacted with catalytic His272 in the active site. Conclusion: Present study explains the binding efficiency and repurposing potential of certain HCV protease inhibitors against to SARS-CoV-2 PLpro enzyme. Docking sites and potential druggability of ligands were also crosschecked by the estimation of druggable pockets. Thereby our results can promote promising preliminary data for research on drug development in the fight of Covid-19.

Synthesis of sterically hindered 3,5,5-trimethyl 2,6-dioxo tetrahydro pyrimidine as HCV protease inhibitors

2010 ◽  
Vol 51 (9) ◽  
pp. 1276-1279 ◽  
Author(s):  
Latha G. Nair ◽  
Stephane Bogen ◽  
Ronald J. Doll ◽  
N.-Y. Shih ◽  
F. George Njoroge
Keyword(s):  
Protease Inhibitors ◽  
Hcv Protease ◽  
Sterically Hindered

scholarly journals Variation analysis of six HCV viral load assays using low viremic HCV samples in the range of the clinical decision points for HCV protease inhibitors

2014 ◽  
Vol 204 (4) ◽  
pp. 515-525 ◽  
Author(s):  
F. Wiesmann ◽  
G. Naeth ◽  
C. Sarrazin ◽  
A. Berger ◽  
R. Kaiser ◽  
...  
Keyword(s):  
Viral Load ◽  
Protease Inhibitors ◽  
Clinical Decision ◽  
Variation Analysis ◽  
Decision Points ◽  
Hcv Protease

Hepatitis C treatment with a focus on HCV protease inhibitors (Part Two)

2013 ◽  
Author(s):  
Philippe Halfon ◽  
Salvatore Petta ◽  
Antonio Craxì
Keyword(s):  
Hepatitis C ◽  
Protease Inhibitors ◽  
Hepatitis C Treatment ◽  
Hcv Protease

scholarly journals Triple therapy with first generation HCV protease inhibitors: Lead-in or no lead-in phase?

2013 ◽  
Vol 58 (2) ◽  
pp. 391-394 ◽  
Author(s):  
Alina Pascale ◽  
Lawrence Serfaty
Keyword(s):  
Triple Therapy ◽  
Protease Inhibitors ◽  
First Generation ◽  
Hcv Protease

20 IN VITRO ACTIVITY AND PHARMACOLOGIC PROPERTIES OF TWO NOVEL SERIES OF HCV PROTEASE INHIBITORS

2008 ◽  
Vol 48 ◽  
pp. S10
Author(s):  
D.N. Standring ◽  
C. Parsy ◽  
F.-R. Alexandre ◽  
M. Derock ◽  
F. Leroy ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Hcv Protease

1195 TEMPORAL DYNAMIC OF MUTATIONS ASSOCIATED WITH HCV PROTEASE INHIBITORS RESISTANCE IN NATURAL STRAINS OF HIV/HCV COINFECTED INDIVIDUALS

2012 ◽  
Vol 56 ◽  
pp. S474
Author(s):  
E. Messina ◽  
S. Bagaglio ◽  
M. Merli ◽  
L. Porrino ◽  
A.R. Pignataro ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Temporal Dynamic ◽  
Hcv Protease ◽  
Natural Strains

P4 and P1′ optimization of bicycloproline P2 bearing tetrapeptidyl α-ketoamides as HCV protease inhibitors

2004 ◽  
Vol 14 (19) ◽  
pp. 5007-5011 ◽  
Author(s):  
Yvonne Yip ◽  
Frantz Victor ◽  
Jason Lamar ◽  
Robert Johnson ◽  
Q. May Wang ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Hcv Protease
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