Target Information
| Target General Infomation | Top | ||||
|---|---|---|---|---|---|
| Target ID |
T87325
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| Target Name |
COVID-19 papain-like proteinase (PL-PRO)
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| Synonyms |
COVID-19 papain-like proteinase; COVID-19 PL2-PRO; COVID-19 PL-PRO; COVID-19 main proteinase; COVID-19 non-structural protein 3
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| Gene Name |
COVID-19 rep; COVID-19 1a-1b
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| Target Status |
Target in Phase 3 Trial
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[1] | |||
| Disease | [+] 1 Target-related Diseases | + | |||
| 1 | COVID-19 [ICD-11: 1D6Y] | ||||
| Function |
Responsible for the cleavages located at the N-terminus of the replicase polyprotein. In addition, PL-PRO possesses a deubiquitinating/deISGylating activity and processes both 'Lys-48'- and 'Lys-63'-linked polyubiquitin chains from cellular substrates. Participates together with nsp4 in the assembly of virally-induced cytoplasmic double-membrane vesicles necessary for viral replication. Antagonizes innate immune induction of type I interferon by blocking the phosphorylation, dimerization and subsequent nuclear translocation of host IRF3. Prevents also host NF-kappa-B signaling.
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| BioChemical Class |
Coronaviruses polyprotein 1ab family
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| UniProt ID | |||||
| EC Number |
EC 3.4.19.12
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| Sequence |
APTKVTFGDDTVIEVQGYKSVNITFELDERIDKVLNEKCSAYTVELGTEVNEFACVVADA
VIKTLQPVSELLTPLGIDLDEWSMATYYLFDESGEFKLASHMYCSFYPPDEDEEEGDCEE EEFEPSTQYEYGTEDDYQGKPLEFGATSAALQPEEEQEEDWLDDDSQQTVGQQDGSEDNQ TTTIQTIVEVQPQLEMELTPVVQTIEVNSFSGYLKLTDNVYIKNADIVEEAKKVKPTVVV NAANVYLKHGGGVAGALNKATNNAMQVESDDYIATNGPLKVGGSCVLSGHNLAKHCLHVV GPNVNKGEDIQLLKSAYENFNQHEVLLAPLLSAGIFGADPIHSLRVCVDTVRTNVYLAVF DKNLYDKLVSSFLEMKSEKQVEQKIAEIPKEEVKPFITESKPSVEQRKQDDKKIKACVEE VTTTLEETKFLTENLLLYIDINGNLHPDSATLVSDIDITFLKKDAPYIVGDVVQEGVLTA VVIPTKKAGGTTEMLAKALRKVPTDNYITTYPGQGLNGYTVEEAKTVLKKCKSAFYILPS IISNEKQEILGTVSWNLREMLAHAEETRKLMPVCVETKAIVSTIQRKYKGIKIQEGVVDY GARFYFYTSKTTVASLINTLNDLNETLVTMPLGYVTHGLNLEEAARYMRSLKVPATVSVS SPDAVTAYNGYLTSSSKTPEEHFIETISLAGSYKDWSYSGQSTQLGIEFLKRGDKSVYYT SNPTTFHLDGEVITFDNLKTLLSLREVRTIKVFTTVDNINLHTQVVDMSMTYGQQFGPTY LDGADVTKIKPHNSHEGKTFYVLPNDDTLRVEAFEYYHTTDPSFLGRYMSALNHTKKWKY PQVNGLTSIKWADNNCYLATALLTLQQIELKFNPPALQDAYYRARAGEAANFCALILAYC NKTVGELGDVRETMSYLFQHANLDSCKRVLNVVCKTCGQQQTTLKGVEAVMYMGTLSYEQ FKKGVQIPCTCGKQATKYLVQQESPFVMMSAPPAQYELKHGTFTCASEYTGNYQCGHYKH ITSKETLYCIDGALLTKSSEYKGPITDVFYKENSYTTTIKPVTYKLDGVVCTEIDPKLDN YYKKDNSYFTEQPIDLVPNQPYPNASFDNFKFVCDNIKFADDLNQLTGYKKPASRELKVT FFPDLNGDVVAIDYKHYTPSFKKGAKLLHKPIVWHVNNATNKATYKPNTWCIRCLWSTKP VETSNSFDVLKSEDAQGMDNLACEDLKPVSEEVVENPTIQKDVLECNVKTTEVVGDIILK PANNSLKITEEVGHTDLMAAYVDNSSLTIKKPNELSRVLGLKTLATHGLAAVNSVPWDTI ANYAKPFLNKVVSTTTNIVTRCLNRVCTNYMPYFFTLLLQLCTFTRSTNSRIKASMPTTI AKNTVKSVGKFCLEASFNYLKSPNFSKLINIIIWFLLLSVCLGSLIYSTAALGVLMSNLG MPSYCTGYREGYLNSTNVTIATYCTGSIPCSVCLSGLDSLDTYPSLETIQITISSFKWDL TAFGLVAEWFLAYILFTRFFYVLGLAAIMQLFFSYFAVHFISNSWLMWLIINLVQMAPIS AMVRMYIFFASFYYVWKSYVHVVDGCNSSTCMMCYKRNRATRVECTTIVNGVRRSFYVYA NGGKGFCKLHNWNCVNCDTFCAGSTFISDEVARDLSLQFKRPINPTDQSSYIVDSVTVKN GSIHLYFDKAGQKTYERHSLSHFVNLDNLRANNTKGSLPINVIVFDGKSKCEESSAKSAS VYYSQLMCQPILLLDQALVSDVGDSAEVAVKMFDAYVNTFSSTFNVPMEKLKTLVATAEA ELAKNVSLDNVLSTFISAARQGFVDSDVETKDVVECLKLSHQSDIEVTGDSCNNYMLTYN KVENMTPRDLGACIDCSARHINAQVAKSHNIALIWNVKDFMSLSEQLRKQIRSAAKKNNL PF |
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| Drugs and Modes of Action | Top | ||||
|---|---|---|---|---|---|
| Drugs in Phase 3 Trial | [+] 1 Drugs in Phase 3 Trial | + | |||
| 1 | Isotretinoin | Drug Info | Phase 3 Trial | COVID-19 | [2] |
| Investigative agents | [+] 9 Investigative agents | + | |||
| 1 | PMID26868298-compound-N3 | Drug Info | Investigative | COVID-19 | [1] |
| 2 | PX-12 | Drug Info | Investigative | COVID-19 | [1] |
| 3 | Hexylcarbamoyl fluorouracil | Drug Info | Investigative | COVID-19 | [1] |
| 4 | SPI-1005 | Drug Info | Investigative | COVID-19 | [1] |
| 5 | Disulfiram | Drug Info | Investigative | COVID-19 | [1] |
| 6 | Isoarnebin 4 | Drug Info | Investigative | COVID-19 | [1] |
| 7 | Tideglusib | Drug Info | Investigative | COVID-19 | [1] |
| 8 | PMID32321856-compound-11a | Drug Info | Investigative | COVID-19 | [3] |
| 9 | PMID32321856-compound-11b | Drug Info | Investigative | COVID-19 | [3] |
| Mode of Action | [+] 1 Modes of Action | + | |||
| Inhibitor | [+] 10 Inhibitor drugs | + | |||
| 1 | Isotretinoin | Drug Info | [2] | ||
| 2 | Disulfiram | Drug Info | [1] | ||
| 3 | SPI-1005 | Drug Info | [1] | ||
| 4 | PMID26868298-compound-N3 | Drug Info | [1] | ||
| 5 | Hexylcarbamoyl fluorouracil | Drug Info | [1] | ||
| 6 | Isoarnebin 4 | Drug Info | [1] | ||
| 7 | PMID32321856-compound-11a | Drug Info | [3] | ||
| 8 | PMID32321856-compound-11b | Drug Info | [3] | ||
| 9 | PX-12 | Drug Info | [1] | ||
| 10 | Tideglusib | Drug Info | [1] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| 1 | Structure of Mpro from COVID-19 virus and discovery of its inhibitors. Nature. 2020 Apr 9. | ||||
| 2 | ClinicalTrials.gov (NCT04361422) Isotretinoin in Treatment of COVID-19. U.S. National Institutes of Health. | ||||
| 3 | Structure-based Design of Antiviral Drug Candidates Targeting the SARS-CoV-2 Main Protease. Science. 2020 Apr 22;eabb4489. | ||||
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