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  1. Article ; Online: FlipGFP protease assay for evaluating in vitro inhibitory activity against SARS-CoV-2 M

    Tan, Haozhou / Hu, Yanmei / Wang, Jun

    STAR protocols

    2023  Volume 4, Issue 2, Page(s) 102323

    Abstract: FlipGFP assay characterizes the intracellular drug target engagement to ... ...

    Abstract FlipGFP assay characterizes the intracellular drug target engagement to M
    Language English
    Publishing date 2023-05-04
    Publishing country United States
    Document type Journal Article
    ISSN 2666-1667
    ISSN (online) 2666-1667
    DOI 10.1016/j.xpro.2023.102323
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  2. Article: Invalidation of dieckol and 1,2,3,4,6-pentagalloylglucose (PGG) as SARS-CoV-2 main protease inhibitors and the discovery of PGG as a papain-like protease inhibitor.

    Tan, Haozhou / Ma, Chunlong / Wang, Jun

    Research square

    2022  

    Abstract: The COVID-19 pandemic spurred a broad interest in antiviral drug discovery. The SARS-CoV-2 main protease ( ... ...

    Abstract The COVID-19 pandemic spurred a broad interest in antiviral drug discovery. The SARS-CoV-2 main protease (M
    Language English
    Publishing date 2022-03-30
    Publishing country United States
    Document type Preprint
    DOI 10.21203/rs.3.rs-1490282/v1
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Invalidation of dieckol and 1,2,3,4,6-pentagalloylglucose (PGG) as SARS-CoV-2 main protease inhibitors and the discovery of PGG as a papain-like protease inhibitor.

    Tan, Haozhou / Ma, Chunlong / Wang, Jun

    Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents

    2022  Volume 31, Issue 7, Page(s) 1147–1153

    Abstract: The COVID-19 pandemic spurred a broad interest in antiviral drug discovery. The SARS-CoV-2 main protease ( ... ...

    Abstract The COVID-19 pandemic spurred a broad interest in antiviral drug discovery. The SARS-CoV-2 main protease (M
    Language English
    Publishing date 2022-05-12
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1116702-6
    ISSN 1054-2523
    ISSN 1054-2523
    DOI 10.1007/s00044-022-02903-0
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  4. Article ; Online: An Overview of Antivirals against Monkeypox Virus and Other Orthopoxviruses.

    Wang, Jun / Shahed-Ai-Mahmud, Md / Chen, Angelo / Li, Kan / Tan, Haozhou / Joyce, Ryan

    Journal of medicinal chemistry

    2023  Volume 66, Issue 7, Page(s) 4468–4490

    Abstract: The current monkeypox outbreaks during the COVID-19 pandemic have reignited interest in orthopoxvirus antivirals. Monkeypox belongs to ... ...

    Abstract The current monkeypox outbreaks during the COVID-19 pandemic have reignited interest in orthopoxvirus antivirals. Monkeypox belongs to the
    MeSH term(s) Animals ; Humans ; Orthopoxvirus ; Monkeypox virus ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; Mpox (monkeypox)/drug therapy ; Pandemics ; COVID-19 ; Variola virus
    Chemical Substances Antiviral Agents
    Language English
    Publishing date 2023-03-24
    Publishing country United States
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c00069
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  5. Article ; Online: SARS-CoV-2 Main Protease Drug Design, Assay Development, and Drug Resistance Studies.

    Tan, Bin / Joyce, Ryan / Tan, Haozhou / Hu, Yanmei / Wang, Jun

    Accounts of chemical research

    2022  Volume 56, Issue 2, Page(s) 157–168

    Abstract: SARS-CoV-2 is the etiological pathogen of the COVID-19 pandemic, which led to more than 6.5 million deaths since the beginning of the outbreak in December 2019. The unprecedented disruption of social life and public health caused by COVID-19 calls for ... ...

    Abstract SARS-CoV-2 is the etiological pathogen of the COVID-19 pandemic, which led to more than 6.5 million deaths since the beginning of the outbreak in December 2019. The unprecedented disruption of social life and public health caused by COVID-19 calls for fast-track development of diagnostic kits, vaccines, and antiviral drugs. Small molecule antivirals are essential complements of vaccines and can be used for the treatment of SARS-CoV-2 infections. Currently, there are three FDA-approved antiviral drugs, remdesivir, molnupiravir, and paxlovid. Given the moderate clinical efficacy of remdesivir and molnupiravir, the drug-drug interaction of paxlovid, and the emergence of SARS-CoV-2 variants with potential drug-resistant mutations, there is a pressing need for additional antivirals to combat current and future coronavirus outbreaks.In this Account, we describe our efforts in developing covalent and noncovalent main protease (M
    MeSH term(s) Humans ; SARS-CoV-2 ; COVID-19 ; Cathepsin L ; Pandemics ; Antiviral Agents/pharmacology ; Antiviral Agents/chemistry ; Drug Design
    Chemical Substances nirmatrelvir and ritonavir drug combination ; molnupiravir (YA84KI1VEW) ; Cathepsin L (EC 3.4.22.15) ; 3C-like proteinase, SARS-CoV-2 (EC 3.4.22.-) ; Antiviral Agents
    Language English
    Publishing date 2022-12-29
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1483291-4
    ISSN 1520-4898 ; 0001-4842
    ISSN (online) 1520-4898
    ISSN 0001-4842
    DOI 10.1021/acs.accounts.2c00735
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  6. Article ; Online: Progress and Challenges in Targeting the SARS-CoV-2 Papain-like Protease.

    Tan, Haozhou / Hu, Yanmei / Jadhav, Prakash / Tan, Bin / Wang, Jun

    Journal of medicinal chemistry

    2022  Volume 65, Issue 11, Page(s) 7561–7580

    Abstract: SARS-CoV-2 is the causative agent of the COVID-19 pandemic. The approval of vaccines and small-molecule antivirals is vital in combating the pandemic. The viral polymerase inhibitors remdesivir and molnupiravir and the viral main protease inhibitor ... ...

    Abstract SARS-CoV-2 is the causative agent of the COVID-19 pandemic. The approval of vaccines and small-molecule antivirals is vital in combating the pandemic. The viral polymerase inhibitors remdesivir and molnupiravir and the viral main protease inhibitor nirmatrelvir/ritonavir have been approved by the U.S. FDA. However, the emergence of variants of concern/interest calls for additional antivirals with novel mechanisms of action. The SARS-CoV-2 papain-like protease (PL
    MeSH term(s) Antiviral Agents/pharmacology ; Coronavirus Papain-Like Proteases ; Humans ; Pandemics ; Protease Inhibitors/pharmacology ; SARS-CoV-2 ; COVID-19 Drug Treatment
    Chemical Substances Antiviral Agents ; Protease Inhibitors ; Coronavirus Papain-Like Proteases (EC 3.4.22.2) ; papain-like protease, SARS-CoV-2 (EC 3.4.22.2)
    Language English
    Publishing date 2022-05-27
    Publishing country United States
    Document type Journal Article ; Review ; Research Support, N.I.H., Extramural
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.2c00303
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  7. Article: Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays.

    Ma, Chunlong / Tan, Haozhou / Choza, Juliana / Wang, Yuyin / Wang, Jun

    Acta pharmaceutica Sinica. B

    2021  Volume 12, Issue 4, Page(s) 1636–1651

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

    Abstract SARS-CoV-2 main protease (M
    Language English
    Publishing date 2021-11-01
    Publishing country Netherlands
    Document type Journal Article
    ISSN 2211-3835
    ISSN 2211-3835
    DOI 10.1016/j.apsb.2021.10.026
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  8. Article ; Online: Telaprevir Treatment Reduces Paralysis in a Mouse Model of Enterovirus D68 Acute Flaccid Myelitis.

    Frost, Joshua / Rudy, Michael J / Leser, J Smith / Tan, Haozhou / Hu, Yanmei / Wang, Jun / Clarke, Penny / Tyler, Kenneth L

    Journal of virology

    2023  Volume 97, Issue 5, Page(s) e0015623

    Abstract: In 2014, 2016, and 2018, the United States experienced unprecedented spikes in pediatric cases of acute flaccid myelitis (AFM), which is a poliomyelitis-like paralytic illness. Accumulating clinical, immunological, and epidemiological evidence has ... ...

    Abstract In 2014, 2016, and 2018, the United States experienced unprecedented spikes in pediatric cases of acute flaccid myelitis (AFM), which is a poliomyelitis-like paralytic illness. Accumulating clinical, immunological, and epidemiological evidence has identified enterovirus D68 (EV-D68) as a major causative agent of these biennial AFM outbreaks. There are currently no available FDA-approved antivirals that are effective against EV-D68, and the treatment for EV-D68-associated AFM is primarily supportive. Telaprevir is an food and drug administration (FDA)-approved protease inhibitor that irreversibly binds the EV-D68 2A protease and inhibits EV-D68 replication
    MeSH term(s) Animals ; United States ; Mice ; Enterovirus D, Human/physiology ; Disease Models, Animal ; Paralysis/drug therapy ; Paralysis/etiology ; Central Nervous System Viral Diseases ; Enterovirus Infections/pathology ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use
    Chemical Substances telaprevir (655M5O3W0U) ; Antiviral Agents
    Language English
    Publishing date 2023-05-08
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 80174-4
    ISSN 1098-5514 ; 0022-538X
    ISSN (online) 1098-5514
    ISSN 0022-538X
    DOI 10.1128/jvi.00156-23
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  9. Article ; Online: Exploring diverse reactive warheads for the design of SARS-CoV-2 main protease inhibitors.

    Tan, Bin / Sacco, Michael / Tan, Haozhou / Li, Kan / Joyce, Ryan / Zhang, Xiujun / Chen, Yu / Wang, Jun

    European journal of medicinal chemistry

    2023  Volume 259, Page(s) 115667

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

    Abstract SARS-CoV-2 main protease (M
    MeSH term(s) Humans ; COVID-19 ; SARS-CoV-2 ; Antiviral Agents/pharmacology ; Nitriles ; Protease Inhibitors/pharmacology
    Chemical Substances 3C-like proteinase, SARS-CoV-2 (EC 3.4.22.-) ; nirmatrelvir and ritonavir drug combination ; Antiviral Agents ; Nitriles ; Protease Inhibitors
    Language English
    Publishing date 2023-07-19
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2023.115667
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  10. Article ; Online: Design of a SARS-CoV-2 papain-like protease inhibitor with antiviral efficacy in a mouse model.

    Tan, Bin / Zhang, Xiaoming / Ansari, Ahmadullah / Jadhav, Prakash / Tan, Haozhou / Li, Kan / Chopra, Ashima / Ford, Alexandra / Chi, Xiang / Ruiz, Francesc Xavier / Arnold, Eddy / Deng, Xufang / Wang, Jun

    Science (New York, N.Y.)

    2024  Volume 383, Issue 6690, Page(s) 1434–1440

    Abstract: The emergence of SARS-CoV-2 variants and drug-resistant mutants calls for additional oral antivirals. The SARS-CoV-2 papain-like protease ( ... ...

    Abstract The emergence of SARS-CoV-2 variants and drug-resistant mutants calls for additional oral antivirals. The SARS-CoV-2 papain-like protease (PL
    MeSH term(s) Animals ; Mice ; Coronavirus Papain-Like Proteases/antagonists & inhibitors ; Coronavirus Papain-Like Proteases/chemistry ; COVID-19 ; Disease Models, Animal ; SARS-CoV-2/drug effects ; SARS-CoV-2/enzymology ; Coronavirus Protease Inhibitors/administration & dosage ; Coronavirus Protease Inhibitors/chemistry ; Coronavirus Protease Inhibitors/pharmacology ; Drug Design ; COVID-19 Drug Treatment ; Administration, Oral ; Crystallography, X-Ray ; Structure-Activity Relationship ; Viral Load/drug effects ; Male ; Mice, Inbred C57BL ; Mice, Inbred BALB C
    Chemical Substances Coronavirus Papain-Like Proteases (EC 3.4.22.2) ; papain-like protease, SARS-CoV-2 (EC 3.4.22.2) ; Coronavirus Protease Inhibitors
    Language English
    Publishing date 2024-03-28
    Publishing country United States
    Document type Journal Article
    ZDB-ID 128410-1
    ISSN 1095-9203 ; 0036-8075
    ISSN (online) 1095-9203
    ISSN 0036-8075
    DOI 10.1126/science.adm9724
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