Target Information
| Target General Infomation | Top | ||||
|---|---|---|---|---|---|
| Target ID |
T89826
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| Target Name |
SARS-CoV 3C-like protease (3CLpro)
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| Synonyms |
SARS-CoV 3C-like protease; SARS-CoV 3CLp; SARS-CoV 3CL-PRO; SARS-CoV 3CLpro
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| Gene Name |
SARS-CoV rep; SARS-CoV 1a-1b
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| Target Status |
Target in Preclinical Study
|
[1] | |||
| Disease | [+] 1 Target-related Diseases | + | |||
| 1 | Severe acute respiratory syndrome [ICD-11: 1D65] | ||||
| Function |
Cleaves the C-terminus of replicase polyprotein at 11 sites. Recognizes substrates containing the core sequence [ILMVF]-Q-|-[SGACN]. Also able to bind an ADP-ribose-1''-phosphate (ADRP). May cleave host ATP6V1G1 thereby modifying host vacuoles intracellular pH.
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| BioChemical Class |
Coronaviruses polyprotein 1ab family
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| UniProt ID | |||||
| EC Number |
EC 3.4.22.-
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| Sequence |
SGFRKMAFPSGKVEGCMVQVTCGTTTLNGLWLDDTVYCPRHVICTAEDMLNPNYEDLLIR
KSNHSFLVQAGNVQLRVIGHSMQNCLLRLKVDTSNPKTPKYKFVRIQPGQTFSVLACYNG SPSGVYQCAMRPNHTIKGSFLNGSCGSVGFNIDYDCVSFCYMHHMELPTGVHAGTDLEGK FYGPFVDRQTAQAAGTDTTITLNVLAWLYAAVINGDRWFLNRFTTTLNDFNLVAMKYNYE PLTQDHVDILGPLSAQTGIAVLDMCAALKELLQNGMNGRTILGSTILEDEFTPFDVVRQC SGVTFQ |
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| Drugs and Modes of Action | Top | ||||
|---|---|---|---|---|---|
| Preclinical Drugs | [+] 9 Preclinical Drugs | + | |||
| 1 | Lopinavir | Drug Info | Preclinical | SARS | [2] |
| 2 | Phenylisoserine derivatives SK80 | Drug Info | Preclinical | SARS | [3] |
| 3 | PMID28216367-compound-6d | Drug Info | Preclinical | SARS | [4] |
| 4 | PMID26868298-compound-N3 | Drug Info | Preclinical | SARS | [2] |
| 5 | PMID30784880-compound-6-5 | Drug Info | Preclinical | SARS | [5] |
| 6 | GC376 | Drug Info | Preclinical | SARS | [6] |
| 7 | PMID27240464-compound-3f | Drug Info | Preclinical | SARS | [7] |
| 8 | GRL-001 | Drug Info | Preclinical | SARS | [2] |
| 9 | PMID28624700-compound-3-31 | Drug Info | Preclinical | SARS | [1] |
| Mode of Action | [+] 1 Modes of Action | + | |||
| Inhibitor | [+] 9 Inhibitor drugs | + | |||
| 1 | GC376 | Drug Info | [6] | ||
| 2 | GRL-001 | Drug Info | [2] | ||
| 3 | Lopinavir | Drug Info | [2] | ||
| 4 | Phenylisoserine derivatives SK80 | Drug Info | [3] | ||
| 5 | PMID26868298-compound-N3 | Drug Info | [2] | ||
| 6 | PMID27240464-compound-3f | Drug Info | [7] | ||
| 7 | PMID28216367-compound-6d | Drug Info | [4] | ||
| 8 | PMID28624700-compound-3-31 | Drug Info | [1] | ||
| 9 | PMID30784880-compound-6-5 | Drug Info | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| 1 | Discovery of Unsymmetrical Aromatic Disulfides as Novel Inhibitors of SARS-CoV Main Protease: Chemical Synthesis, Biological Evaluation, Molecular Docking and 3D-QSAR Study Eur J Med Chem. 2017 Sep 8;137:450-461. | ||||
| 2 | Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47. | ||||
| 3 | Synthesis and Evaluation of Phenylisoserine Derivatives for the SARS-CoV 3CL Protease Inhibitor. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2746-2751. | ||||
| 4 | Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors. Antiviral Res. 2017 May;141:101-106. | ||||
| 5 | Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives. Eur J Med Chem. 2019 Apr 1;167:472-484. | ||||
| 6 | Reversal of the Progression of Fatal Coronavirus Infection in Cats by a Broad-Spectrum Coronavirus Protease Inhibitor. PLoS Pathog. 2016 Mar 30;12(3):e1005531. | ||||
| 7 | Identification, synthesis and evaluation of SARS-CoV and MERS-CoV 3C-like protease inhibitors. Bioorg Med Chem. 2016 Jul 1;24(13):3035-3042. | ||||
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