Target Information | Therapeutic Target Database

Target General Information

Target ID

T89826

Target Name

SARS-CoV 3C-like protease (3CLpro)

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

Disease

[+] 1 Target-related Diseases

+

1

Human immunodeficiency virus disease [ICD-11: 1C60-1C62]

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

UniProt ID

R1AB_CVHSA (3241-3546)

EC Number

EC 3.4.22.-

Sequence

SGFRKMAFPSGKVEGCMVQVTCGTTTLNGLWLDDTVYCPRHVICTAEDMLNPNYEDLLIR
KSNHSFLVQAGNVQLRVIGHSMQNCLLRLKVDTSNPKTPKYKFVRIQPGQTFSVLACYNG
SPSGVYQCAMRPNHTIKGSFLNGSCGSVGFNIDYDCVSFCYMHHMELPTGVHAGTDLEGK
FYGPFVDRQTAQAAGTDTTITLNVLAWLYAAVINGDRWFLNRFTTTLNDFNLVAMKYNYE
PLTQDHVDILGPLSAQTGIAVLDMCAALKELLQNGMNGRTILGSTILEDEFTPFDVVRQC
SGVTFQ

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3D Structure

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PDB

Drugs and Modes of Action

Preclinical Drugs

[+] 9

+

1

Lopinavir

Drug Info

Approved

Human immunodeficiency virus infection

[2]

2

GC376

Drug Info

Preclinical

Severe acute respiratory syndrome (SARS)

[3]

3

GRL-001

Drug Info

Preclinical

Severe acute respiratory syndrome (SARS)

[4]

4

Phenylisoserine derivatives SK80

Drug Info

Preclinical

Severe acute respiratory syndrome (SARS)

[5]

5

PMID26868298-compound-N3

Drug Info

Preclinical

Severe acute respiratory syndrome (SARS)

[4]

6

PMID27240464-compound-3f

Drug Info

Preclinical

Severe acute respiratory syndrome (SARS)

[6]

7

PMID28216367-compound-6d

Drug Info

Preclinical

Severe acute respiratory syndrome (SARS)

[7]

8

PMID28624700-compound-3-31

Drug Info

Preclinical

Severe acute respiratory syndrome (SARS)

[1]

9

PMID30784880-compound-6-5

Drug Info

Preclinical

Severe acute respiratory syndrome (SARS)

[8]

Mode of Action

[+] 1 Modes of Action

+

Inhibitor

[+] 9 Inhibitor drugs

+

1

GC376

Drug Info

[3]

2

GRL-001

Drug Info

[4]

3

Lopinavir

Drug Info

[4]

4

Phenylisoserine derivatives SK80

Drug Info

[5]

5

PMID26868298-compound-N3

Drug Info

[4]

6

PMID27240464-compound-3f

Drug Info

[6]

7

PMID28216367-compound-6d

Drug Info

[7]

8

PMID28624700-compound-3-31

Drug Info

[1]

9

PMID30784880-compound-6-5

Drug Info

[8]

Chemical Structure based Activity Landscape of Target

References

REF 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.

REF 2

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 3

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.

REF 4

Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47.

REF 5

Synthesis and Evaluation of Phenylisoserine Derivatives for the SARS-CoV 3CL Protease Inhibitor. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2746-2751.

REF 6

Identification, synthesis and evaluation of SARS-CoV and MERS-CoV 3C-like protease inhibitors. Bioorg Med Chem. 2016 Jul 1;24(13):3035-3042.

REF 7

Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors. Antiviral Res. 2017 May;141:101-106.

REF 8

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.

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