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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 | Nat Genet:单基因突变导致过敏性皮炎的发生显示文摘最近,研究者们鉴定出了一类导致神经性皮炎发生的关键基因突变:CARDll。来自美国NIH过敏与传染病研究所的研究者们通过对四个没有血缘关系的患病家庭进行分析,发现了这一导致疾病产生的基因、 | Chi A Ma, Yuan Zhang, Michael A Weinreich, Jonathan J Lyons, Celeste G Nelson, Thomas DiMaggio, Kelly D Stone, Joshua D Milner Jeffrey R Stinson, Elisa Ruffo, Batsukh Dorjbal, Swadhinya Arjunaraja, Kelsey Voss, Andrew L Snow Jordan K Abbott, Pia J Hauk, Paul R Reynolds, Erwin W Gelfand Elisa Ruffo Salomé Glauzy, Natsuko Yamakawa, Eric Meffre Jennifer Stoddard, Julie Niemela, Sergio D Rosenzweig Yu Zhang, Helen F Matthews Joshua J McElwee Nina Jones Alejandro Palma, Matías Oleastro, Emma Prieto, Andrea R Bernasconi, Geronimo Dubra, Silvia Danielian, Jonathan Zaiat, Marcelo A Marti Brian Kim Megan A Cooper Neil Romberg | 2017 | 现代生物医学进展2017，17，27： | 3 |
| 3 | Human Embryonic Stem Cells Derived by Somatic Cell Nuclear Transfer显示文摘 | Masahito Tachibana Paula Amato Michelle Sparman Nuria Marti Gutierrez Rebecca Tippner-Hedges Hong Ma Eunju Kang Alimujiang Fulati Hyo-Sang Lee Hathaitip Sritanaudomchai Keith Masterson Janine Larson Deborah Eaton Karen Sadler-Fredd David Battaglia David L | 2013 | Cell2013，，6： | 2 |
| 4 | Inflammation and conjugated linoleic acid: mechanisms of action and implications for human health显示文摘 | Zulet MA Marti A Parra MD | 2005 | J Physiol Biochem2005，61，3： | 1 |
| 5 | Leptin gene transfer into muscle increases lipolysis and oxygen consumption in white fat tissue in ob/ob mice 显示文摘 | Marti A Novo FJ Eduardo MA et d | 1998 | Biochem Biophy Res Comm1998，246，3： | 1 |
| 6 | SarA is an essential positive regulator of Staphylococcus epiderrnidis biofilm development 显示文摘 | Tormo MA Marti M Valle J | 2005 | J Bacteriol2005，187，7： | 1 |
| 7 | Comparative study of two models that use biochemical parameters for the noninvasive diagnosis of fibrosis in patients with hepatitis C显示文摘 | Romero Gomez M Rami rez Marti n del Campo M Otero MA | 2005 | Med Clin2005，124，20： | 1 |
| 8 | In vivo antitumor activity of NVP-AEW541-a novel, potent, and se lective inhibitor of the IGF-IR kinase显示文摘 | Garcia-Echeverria C Pearson MA Marti A | 2004 | Cancer Cell2004，5，3： | 1 |
| 9 | Atorvastatin reduces the expression of cyclooxygenase 2 in a rabbit model of atheroselerosis and in culturedvascularsmoothmuscle cells显示文摘 | Hernandez-Presa MA Marti Ventura JL Ortego M | 2002 | Atherosclerosis2002，160，： | 1 |
| 10 | TRP64ARG polymorphism of the beta 3-adrenergic receptor gene and obesity risk:effect modification by a sedentary lifestyle显示文摘 | Marti A Corbalan MS Martinez-Gonzalez MA | 2002 | Diabetes Obes Metab2002，4，6： | 1 |
| 11 | Inflammation and conjugated linoleic acid:mechanisms of action and implications for human health显示文摘 | Zulet MA Marti A Parra MD | 2005 | J Physiol Biochem2005，61，3： | 1 |
| 12 | Factors predicting efficacy of oxaliplatin in combination with 5-fluorouracil(5-FU)+/-folinic acid in a compassionate-use cihort of 481 5-FU-resistant advanced colorectal cancer patients显示文摘 | Bensmaine MA Marty M de Gramont A | 2001 | Br J Cancer2001，85，4： | 1 |
| 13 | Leptin gene transfer into muscle increases lipolysis and oxygen consumption in white fat tissue in ob/ob mice 显示文摘 | Marti A Novo E J Fduardo MA | 1998 | Biochem Biophy Res Comm1998，246，3： | 1 |
| 14 | Long pulse Nd: YAG laser for treatment of leg veins in 40 patients with assessments at 6 and 12 months 显示文摘 | Trells MA Allones I Marti n-V6 zquez MJ | 2004 | Lasers Surg Med2004，35，1： | 1 |
| 15 | In vivo antitumor activity of NVP-AEW-541 A novel, potent, and selective inhibitor of the IGFIR kinase显示文摘 | Garcia Echeverria C Pearson MA Marti A | 2004 | Cancer Cell2004，5，2： | 1 |
| 16 | Sara is an essential positive regulator of Staphylococcus epidermidis biofilm development显示文摘 | Tormo MA Marti M Valle J | 2005 | J Bacteriol2005，187，7： | 1 |
| 17 | Mangnetic resonance imaging of the pharynx in OSA patients and healthy subjectsb显示文摘 | Ciscar MA Juan G Marti nez V | 2001 | Eur Respir J2001，17，1： | 1 |
| 18 | Clinical efficacy and safety of budesonide-formoterol in non-cystic fibrosis bronchiectasis显示文摘 | Marti nez-Garci a MA Soler-Catalufia JJ Catal6 n-Serra P | 2012 | Chest Journal2012，141，2： | 1 |
| 19 | TRP64ARG polymorphism of the beta 3-adrenergic receptor gene and obesity risk:effect modification by a sedentary lifestyle显示文摘 | MARTI A CORBALAN MS MARTINEZ-GONZALEZ MA | 2002 | Diabetes Obes Metab2002，4，： | 1 |
| 20 | Relationships among dis- positional coping strategies, suicidal ideation, and protective factors a- gainst suicide in older adults 显示文摘 | MARTY MA SEGAL DL COOLIDGE FL | 2010 | Aging Mental Health2010，14，8： | 1 |
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