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| 1 | Boceprevir,GC-376,and calpain inhibitors Ⅱ,Ⅻ inhibit SARS-CoV-2 viral replication by targeting the viral main protease显示文摘A new coronavirus SARS-CoV-2,also called novel coronavirus 2019(2019-nCoV),started to circulate among humans around December 2019,and it is now widespread as a global pandemic.The disease caused by SARS-CoV-2 virus is called COVID-19,which is highly contagious and has an overall mortality rate of 6.35%as of May 26,2020.There is no vaccine or antiviral available for SARS-CoV-2.In this study,we report our discovery of inhibitors targeting the SARS-CoV-2 main protease(Mpro).Using the FRET-based enzymatic assay,several inhibitors including boceprevir,GC-376,and calpain inhibitorsⅡ,andⅫwere identified to have potent activity with single-digit to submicromolar ICs0 values in the enzymatic assay.The mechanism of action of the hits was further characterized using enzyme kinetic studies,thermal shift binding assays,and native mass spectrometry.Significantly,four compounds(boceprevir,GC-376,calpain inhibitorsⅡandⅫ)inhibit SARS-CoV-2 viral replication in cell culture with EC50 values ranging from 0.49 to 3.37μM.Notably,boceprevir,calpain inhibitorsⅡandⅫrepresent novel chemotypes that are distinct from known substrate-based peptidomimetic Mpro inhibitors.A complex crystal structure of SARS-CoV-2 Mpro with GC-376,determined at 2.15(A)resolution with three protomers per asymmetric unit,revealed two unique binding configurations,shedding light on the molecular interactions and protein conformational flexibility underlying substrate and inhibitor binding by Mpro.Overall,the compounds identified herein provide promising starting points for the further development of SARS-CoV-2 therapeutics. | Chunlong Ma Michael Dominic Sacco Brett Hurst Julia Alma Townsend Yanmei Hu Tommy Szeto Xiujun Zhang Bart Tarbet Michael Thomas Marty Yu Chen Jun Wang | 2020 | Cell Research2020，30，8： | 13 |
| 2 | Enhancement of neuromuscular recovery after nerve repair in primates 显示文摘 | Badala mente MA Hurst LC Paul SB | 1987 | J Hand Surg1987，12，2： | 2 |
| 3 | Complete genomes of two clinical Staphylococcus aureus strains:evidence for the rapid evolution of virulence and drug resistance显示文摘 | Holden MT Feil EJ Lindsay JA Peacock SJ Day NP Enright MC Foster TJ Moore CE Hurst L Atkin R Barron A Bason N Bentley SD Chillingworth C Chillingworth T Churcher C Clark L Corton C Cronin A Doggett J Dowd L Feltwell T Hance Z Harris B Hauser H Holroyd S Jagels K James KD Lennard N Line A Mayes R Moule S Mungall K Ormond D Quail MA Rabbinowitsch E Rutherford K Sanders M Sharp S Simmonds M Stevens K Whitehead S Barrell BG Spratt BG Parkhill J | 2004 | Proc Natl Acad Sci USA2004，101，26： | 1 |
| 4 | Improved genome annotation for Zymomonasmobilis 显示文摘 | Yang S Pappas KM Hauser LJ Land ML Chen GL Hurst GB PanC Kouvelis VN Typas MA Pelletier DA Klinqeman DM Chanq YJ Samatova NF Brown SD | 2009 | Nat Biotechnol2009，27，10： | 1 |
| 5 | Reactive skin decon-tamination lotion (RSDL) for the decontamination of chemical warfare agent (CWA) dermal exposure显示文摘 | Schwartz MD Hurst CG Kirk MA | | 0，，10： | 1 |
| 6 | Molecular networksdiscriminating mouse bladder responses to intravesical bacillusCalmette-Guerin(BCG),LPS,and TNF-alpha显示文摘 | Saban MR O'Donnell MA Hurst RE | 2008 | BMC Immunol2008，11，9： | 1 |
| 7 | Reactive skin decon- tamination lotion (RSDL) for the decontamination of chemical warfare agent (CWA) dermal exposure显示文摘 | Schwartz MD Hurst CG Kirk MA | 2012 | Curr Pharm Biotech- nol2012，13，10： | 1 |
| 8 | Molecular biology of bladder cancer:new insights into pathogenesis and clinical diver-sity显示文摘 | Knowles MA Hurst CO | 2015 | Nat Rev Cancer2015，15，1： | 1 |
| 9 | The role of transforming growth factor beta in Dupuytren's disease显示文摘 | Badalamente MA Sampson SP Hurst LC | 1996 | J Hand Surg1996，21，2： | 1 |
| 10 | Injectable collagenase clostridium histolyticum for Dupuytren's contracture显示文摘 | Hurst LC Badalamente MA Hentz VR | 2009 | N Engl J Med2009，361，： | 1 |
| 11 | Pathobiology of the human Al pulley in trigger finger显示文摘 | Sampson SP Badalamente MA Hurst LC | 1991 | J Hand Surg1991，16，： | 1 |
| 12 | Protegrin-1: a broad-spectrum,rapidly microbicidal peptide with in vivo activity显示文摘 | Steinberg DA Hurst MA Fujii CA | 1997 | Antimicrobial Agents and Chemotherapy1997，41，： | 1 |
| 13 | Protegrin-l: a broad-spectrum, rapidly microbicidal peptide with in vivo activity显示文摘 | Steinberg DA Hurst MA Fujii CA | 1997 | Antimicrobial Agents and Chemotherapy1997，41，8： | 1 |
| 14 | Caspase-3,TUNEL and ultra- structural studies of small follicles in adult human ovarian biopsies 显示文摘 | Hurst PR Mora JM Fenwick MA | 2006 | Human Reproduction2006，21，8： | 1 |
| 15 | Pathobiology of the human A1 pulley in trigger finger显示文摘 | SAMPSON SP BADALAMENTE MA HURST LC | 1991 | J Hand Surg Am1991，16，4： | 1 |
| 16 | Antibody blockade of c-fms suppresses the progression of inflammation and injury in early diabetic nephropathy in obese db/db mice显示文摘 | A. K. H. Lim F. Y. Ma D. J. Nikolic-Paterson M. C. Thomas L. A. Hurst G. H. Tesch | 2009 | Diabetologia2009，，8： | 1 |
| 17 | Protegrin-I : a broad-spectrum, rapidly microbicidal peptide with in vivo activity显示文摘 | Steinberg DA Hurst MA Fujii CA | 1997 | Antimicrobial Agents and Chemotherapy1997，41，8： | 1 |
| 18 | Mycobacterium marinum infections of the hand显示文摘 | Hurst LC Amadio PC Badalamente MA | 1987 | J hand Surg Am1987，12，： | 1 |
| 19 | Antibody blockade of c-fms suppresses the progression of inflammation and injury in early diabetic nephropathy in obese db/db mice显示文摘 | A. K. H. Lim F. Y. Ma D. J. Nikolic-Paterson M. C. Thomas L. A. Hurst G. H. Tesch | 2009 | Diabetologia2009，，8： | 1 |
| 20 | Injectable collagenase clostridium histolyticum for Dupuytrenr s contracture显示文摘 | Hurst LC Badalamente MA Hentz VR | 2009 | N Engl J Med2009，361，： | 1 |
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