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Article ; Online: Boceprevir, Calpain Inhibitors II and XII, and GC-376 Have Broad-Spectrum Antiviral Activity against Coronaviruses.

Hu, Yanmei / Ma, Chunlong / Szeto, Tommy / Hurst, Brett / Tarbet, Bart / Wang, Jun

ACS infectious diseases

2021 Volume 7, Issue 3, Page(s) 586–597

Abstract: As the COVID-19 pandemic continues to unfold, the morbidity and mortality are increasing daily. Effective treatment for SARS-CoV-2 is urgently needed. We recently discovered four SARS-CoV-2 main protease ( ... ...

Abstract	As the COVID-19 pandemic continues to unfold, the morbidity and mortality are increasing daily. Effective treatment for SARS-CoV-2 is urgently needed. We recently discovered four SARS-CoV-2 main protease (M
MeSH term(s)	Adenosine Monophosphate/analogs & derivatives ; Adenosine Monophosphate/pharmacology ; Alanine/analogs & derivatives ; Alanine/pharmacology ; Animals ; Antiviral Agents/pharmacology ; Caco-2 Cells ; Carbonates/pharmacology ; Cathepsin L/antagonists & inhibitors ; Cell Line ; Chlorocebus aethiops ; Coronavirus 229E, Human/drug effects ; Coronavirus 3C Proteases/antagonists & inhibitors ; Coronavirus NL63, Human/drug effects ; Coronavirus OC43, Human/drug effects ; Drug Combinations ; Glycoproteins/pharmacology ; HEK293 Cells ; Humans ; Leucine/pharmacology ; Middle East Respiratory Syndrome Coronavirus/drug effects ; Oligopeptides/pharmacology ; Proline/analogs & derivatives ; Proline/pharmacology ; SARS-CoV-2/drug effects ; Serine Endopeptidases/metabolism ; Sulfonic Acids/pharmacology ; Vero Cells ; COVID-19 Drug Treatment
Chemical Substances	Antiviral Agents ; Carbonates ; Drug Combinations ; Glycoproteins ; Oligopeptides ; Sulfonic Acids ; calpain inhibitors ; calpain inhibitor 2 (110115-07-6) ; remdesivir (3QKI37EEHE) ; Adenosine Monophosphate (415SHH325A) ; N-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide (89BT58KELH) ; Proline (9DLQ4CIU6V) ; Serine Endopeptidases (EC 3.4.21.-) ; transmembrane serine protease 2, human (EC 3.4.21.-) ; Cathepsin L (EC 3.4.22.15) ; Coronavirus 3C Proteases (EC 3.4.22.28) ; Leucine (GMW67QNF9C) ; GC376 (H1NMJ5XDG5) ; Alanine (OF5P57N2ZX)
Language	English
Publishing date	2021-03-01
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ISSN	2373-8227
ISSN (online)	2373-8227
DOI	10.1021/acsinfecdis.0c00761
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Boceprevir, calpain inhibitors II and XII, and GC-376 have broad-spectrum antiviral activity against coronaviruses in cell culture.

Hu, Yanmei / Ma, Chunlong / Szeto, Tommy / Hurst, Brett / Tarbet, Bart / Wang, Jun

bioRxiv : the preprint server for biology

2020

Abstract: As the COVID-19 pandemic continues to fold out, the morbidity and mortality are increasing daily. Effective treatment for SARS-CoV-2 is urgently needed. We recently discovered four SARS-CoV-2 main protease (Mpro) inhibitors including boceprevir, calpain ... ...

Abstract	As the COVID-19 pandemic continues to fold out, the morbidity and mortality are increasing daily. Effective treatment for SARS-CoV-2 is urgently needed. We recently discovered four SARS-CoV-2 main protease (Mpro) inhibitors including boceprevir, calpain inhibitors II and XII and GC-376 with potent antiviral activity against infectious SARS-CoV-2 in cell culture. Despite the weaker enzymatic inhibition of calpain inhibitors II and XII against Mpro compared to GC-376, calpain inhibitors II and XII had more potent cellular antiviral activity. This observation promoted us to hypothesize that the cellular antiviral activity of calpain inhibitors II and XII might also involve the inhibition of cathepsin L in addition to Mpro. To test this hypothesis, we tested calpain inhibitors II and XII in the SARS-CoV-2 pseudovirus neutralization assay in Vero E6 cells and found that both compounds significantly decreased pseudoviral particle entry into cells, indicating their role in inhibiting cathepsin L. The involvement of cathepsin L was further confirmed in the drug time-of-addition experiment. In addition, we found that these four compounds not only inhibit SARS-CoV-2, but also SARS-CoV, MERS-CoV, as well as human coronaviruses (CoVs) 229E, OC43, and NL63. The mechanism of action is through targeting the viral Mpro, which was supported by the thermal shift binding assay and enzymatic FRET assay. We further showed that these four compounds have additive antiviral effect when combined with remdesivir. Altogether, these results suggest that boceprevir, calpain inhibitors II and XII, and GC-376 are not only promising antiviral drug candidates against existing human coronaviruses, but also might work against future emerging CoVs.
Keywords	covid19
Language	English
Publishing date	2020-11-01
Publishing country	United States
Document type	Preprint
DOI	10.1101/2020.10.30.362335
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.

Xia, Zilei / Sacco, Michael / Hu, Yanmei / Ma, Chunlong / Meng, Xiangzhi / Zhang, Fushun / Szeto, Tommy / Xiang, Yan / Chen, Yu / Wang, Jun

ACS pharmacology & translational science

2021 Volume 4, Issue 4, Page(s) 1408–1421

Abstract: SARS-CoV-2 main protease ( ... ...

Abstract	SARS-CoV-2 main protease (M
Language	English
Publishing date	2021-06-09
Publishing country	United States
Document type	Journal Article
ISSN	2575-9108
ISSN (online)	2575-9108
DOI	10.1021/acsptsci.1c00099
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease

Ma, Chunlong / Hurst, Brett / Hu, Yanmei / Szeto, Tommy / Tarbet, Bart / Wang, Jun

bioRxiv

Abstract: A novel coronavirus SARS-CoV-2, also called novel coronavirus 2019 (nCoV-19), 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 ... ...

Abstract	A novel coronavirus SARS-CoV-2, also called novel coronavirus 2019 (nCoV-19), 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 6.4% as of April 15, 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, calpain inhibitors II, XII, and MG-132 were identified to have potent activity with single-digit to submicromolar IC50 values in the enzymatic assay. The mechanism of action of the hits was further characterized using enzyme kinetic studies and thermal shift binding assays. Significantly, four compounds (boceprevir, GC-376, calpain inhibitors II and XII) inhibit SARS-CoV-2 viral replication in cell culture with EC50 values ranging from 0.49 to 3.37 micromolar. Notably, boceprevir, calpain inhibitors II and XII represent novel chemotypes that are distinct from known Mpro inhibitors. Overall, the compounds identified herein provide promising starting points for the further development of SARS-CoV-2 therapeutics.
Keywords	covid19
Language	English
Publishing date	2020-04-20
Publisher	Cold Spring Harbor Laboratory
Document type	Article ; Online
DOI	10.1101/2020.04.20.051581
Database	COVID19

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Article ; Online: Boceprevir, calpain inhibitors II and XII, and GC-376 have broad-spectrum antiviral activity against coronaviruses in cell culture

Hu, Yanmei / Ma, Chunlong / Szeto, Tommy / Hurst, Brett / Tarbet, Bart / Wang, Jun

bioRxiv

Abstract	As the COVID-19 pandemic continues to fold out, the morbidity and mortality are increasing daily. Effective treatment for SARS-CoV-2 is urgently needed. We recently discovered four SARS-CoV-2 main protease (Mpro) inhibitors including boceprevir, calpain inhibitors II and XII and GC-376 with potent antiviral activity against infectious SARS-CoV-2 in cell culture. Despite the weaker enzymatic inhibition of calpain inhibitors II and XII against Mpro compared to GC-376, calpain inhibitors II and XII had more potent cellular antiviral activity. This observation promoted us to hypothesize that the cellular antiviral activity of calpain inhibitors II and XII might also involve the inhibition of cathepsin L in addition to Mpro. To test this hypothesis, we tested calpain inhibitors II and XII in the SARS-CoV-2 pseudovirus neutralization assay in Vero E6 cells and found that both compounds significantly decreased pseudoviral particle entry into cells, indicating their role in inhibiting cathepsin L. The involvement of cathepsin L was further confirmed in the drug time-of-addition experiment. In addition, we found that these four compounds not only inhibit SARS-CoV-2, but also SARS-CoV, MERS-CoV, as well as human coronaviruses (CoVs) 229E, OC43, and NL63. The mechanism of action is through targeting the viral Mpro, which was supported by the thermal shift binding assay and enzymatic FRET assay. We further showed that these four compounds have additive antiviral effect when combined with remdesivir. Altogether, these results suggest that boceprevir, calpain inhibitors II and XII, and GC-376 are not only promising antiviral drug candidates against existing human coronaviruses, but also might work against future emerging CoVs.
Keywords	covid19
Language	English
Publishing date	2020-11-01
Publisher	Cold Spring Harbor Laboratory
Document type	Article ; Online
DOI	10.1101/2020.10.30.362335
Database	COVID19

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Article: Discovery of SARS-CoV-2 papain-like protease inhibitors through a combination of high-throughput screening and FlipGFP-based reporter assay.

Xia, Zilei / Sacco, Michael Dominic / Ma, Chunlong / Townsend, Julia Alma / Kitamura, Naoya / Hu, Yanmei / Ba, Mandy / Szeto, Tommy / Zhang, Xiujun / Meng, Xiangzhi / Zhang, Fushun / Xiang, Yan / Marty, Michael Thomas / Chen, Yu / Wang, Jun

bioRxiv : the preprint server for biology

2021

Abstract: The papain-like protease ( ... ...

Abstract	The papain-like protease (PL
Language	English
Publishing date	2021-03-16
Publishing country	United States
Document type	Preprint
DOI	10.1101/2021.03.15.435551
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease.

Ma, Chunlong / Sacco, Michael D / Hurst, Brett / Townsend, Julia A / Hu, Yanmei / Szeto, Tommy / Zhang, Xiujun / Tarbet, Bart / Marty, Michael T / Chen, Yu / Wang, Jun

bioRxiv : the preprint server for biology

2020

Abstract	A novel coronavirus SARS-CoV-2, also called novel coronavirus 2019 (nCoV-19), 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 6.96% as of May 4, 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 (M
Keywords	covid19
Language	English
Publishing date	2020-01-06
Publishing country	United States
Document type	Preprint
DOI	10.1101/2020.04.20.051581
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease.

Ma, Chunlong / Sacco, Michael Dominic / Hurst, Brett / Townsend, Julia Alma / Hu, Yanmei / Szeto, Tommy / Zhang, Xiujun / Tarbet, Bart / Marty, Michael Thomas / Chen, Yu / Wang, Jun

Cell research

2020 Volume 30, Issue 8, Page(s) 678–692

Abstract: 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 ... ...

Abstract	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 (M
MeSH term(s)	A549 Cells ; Animals ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Betacoronavirus/enzymology ; COVID-19 ; Caco-2 Cells ; Chlorocebus aethiops ; Coronavirus 3C Proteases ; Coronavirus Infections/metabolism ; Coronavirus Infections/virology ; Cysteine Endopeptidases/chemistry ; Cysteine Endopeptidases/metabolism ; Drug Discovery/methods ; Glycoproteins/pharmacology ; Humans ; Inhibitory Concentration 50 ; Kinetics ; Pandemics ; Pneumonia, Viral/metabolism ; Pneumonia, Viral/virology ; Proline/analogs & derivatives ; Proline/pharmacology ; Protein Conformation ; Pyrrolidines/chemistry ; Pyrrolidines/pharmacology ; SARS-CoV-2 ; Sulfonic Acids ; Vero Cells ; Viral Nonstructural Proteins/antagonists & inhibitors ; Viral Nonstructural Proteins/chemistry ; Viral Nonstructural Proteins/metabolism ; Virus Replication/drug effects
Chemical Substances	Antiviral Agents ; Glycoproteins ; Pyrrolidines ; Sulfonic Acids ; Viral Nonstructural Proteins ; calpain inhibitors ; N-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide (89BT58KELH) ; Proline (9DLQ4CIU6V) ; Cysteine Endopeptidases (EC 3.4.22.-) ; Coronavirus 3C Proteases (EC 3.4.22.28) ; GC376 (H1NMJ5XDG5)
Keywords	covid19
Language	English
Publishing date	2020-06-15
Publishing country	England
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	1319303-x
ISSN	1748-7838 ; 1001-0602
ISSN (online)	1748-7838
ISSN	1001-0602
DOI	10.1038/s41422-020-0356-z
Database	MEDical Literature Analysis and Retrieval System OnLINE

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

Ma, Chunlong / Sacco, Michael Dominic / Xia, Zilei / Lambrinidis, George / Townsend, Julia Alma / Hu, Yanmei / Meng, Xiangzhi / Szeto, Tommy / Ba, Mandy / Zhang, Xiujun / Gongora, Maura / Zhang, Fushun / Marty, Michael Thomas / Xiang, Yan / Kolocouris, Antonios / Chen, Yu / Wang, Jun

ACS central science

2021 Volume 7, Issue 7, Page(s) 1245–1260

Abstract: The papain-like protease ( ... ...

Abstract	The papain-like protease (PL
Language	English
Publishing date	2021-06-18
Publishing country	United States
Document type	Journal Article
ISSN	2374-7943
ISSN	2374-7943
DOI	10.1021/acscentsci.1c00519
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors.

Kitamura, Naoya / Sacco, Michael Dominic / Ma, Chunlong / Hu, Yanmei / Townsend, Julia Alma / Meng, Xiangzhi / Zhang, Fushun / Zhang, Xiujun / Ba, Mandy / Szeto, Tommy / Kukuljac, Adis / Marty, Michael Thomas / Schultz, David / Cherry, Sara / Xiang, Yan / Chen, Yu / Wang, Jun

Journal of medicinal chemistry

2021 Volume 65, Issue 4, Page(s) 2848–2865

Abstract: The main protease ( ... ...

Abstract	The main protease (M
MeSH term(s)	Animals ; Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; COVID-19/metabolism ; Chlorocebus aethiops ; Coronavirus 3C Proteases/antagonists & inhibitors ; Coronavirus 3C Proteases/isolation & purification ; Coronavirus 3C Proteases/metabolism ; Cysteine Proteinase Inhibitors/chemical synthesis ; Cysteine Proteinase Inhibitors/chemistry ; Cysteine Proteinase Inhibitors/pharmacology ; Dose-Response Relationship, Drug ; Drug Design ; Humans ; Microbial Sensitivity Tests ; Models, Molecular ; Molecular Structure ; Proline/analogs & derivatives ; Proline/chemical synthesis ; Proline/chemistry ; Proline/pharmacology ; Pyrrolidines/chemical synthesis ; Pyrrolidines/chemistry ; Pyrrolidines/pharmacology ; SARS-CoV-2/drug effects ; SARS-CoV-2/enzymology ; Sulfonic Acids/chemical synthesis ; Sulfonic Acids/chemistry ; Sulfonic Acids/pharmacology ; Vero Cells ; COVID-19 Drug Treatment
Chemical Substances	Antiviral Agents ; Cysteine Proteinase Inhibitors ; Pyrrolidines ; Sulfonic Acids ; N-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide (89BT58KELH) ; Proline (9DLQ4CIU6V) ; 3C-like proteinase, SARS-CoV-2 (EC 3.4.22.-) ; Coronavirus 3C Proteases (EC 3.4.22.28) ; GC376 (H1NMJ5XDG5)
Language	English
Publishing date	2021-04-23
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, P.H.S.
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.1c00509
Database	MEDical Literature Analysis and Retrieval System OnLINE

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