Target Information
| Target General Information | Top | |||||
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| Target ID |
T89592
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| Target Name |
MERS-CoV 3C-like proteinase (3CLpro)
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| Synonyms |
MERS-CoV 3C-like proteinase; MERS-CoV 3CLp; MERS-CoV 3CL-PRO; MERS-CoV 3CLpro
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| Gene Name |
MERS-CoV rep; MERS-CoV 1a-1b
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| 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).
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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 |
SGLVKMSHPSGDVEACMVQVTCGSMTLNGLWLDNTVWCPRHVMCPADQLSDPNYDALLIS
MTNHSFSVQKHIGAPANLRVVGHAMQGTLLKLTVDVANPSTPAYTFTTVKPGAAFSVLAC YNGRPTGTFTVVMRPNYTIKGSFLCGSCGSVGYTKEGSVINFCYMHQMELANGTHTGSAF DGTMYGAFMDKQVHQVQLTDKYCSVNVVAWLYAAILNGCAWFVKPNRTSVVSFNEWALAN QFTEFVGTQSVDMLAVKTGVAIEQLLYAIQQLYTGFQGKQILGSTMLEDEFTPEDVNMQI MGVVMQ Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Preclinical Drugs | [+] 7 | + | ||||
| 1 | Lopinavir | Drug Info | Approved | Human immunodeficiency virus infection | [2] | |
| 2 | GC376 | Drug Info | Preclinical | Severe acute respiratory syndrome (SARS) | [5] | |
| 3 | GC813 | Drug Info | Preclinical | Middle East Respiratory Syndrome (MERS) | [1] | |
| 4 | GRL-001 | Drug Info | Preclinical | Severe acute respiratory syndrome (SARS) | [6] | |
| 5 | PMID26868298-compound-N3 | Drug Info | Preclinical | Severe acute respiratory syndrome (SARS) | [6] | |
| 6 | PMID27240464-compound-3f | Drug Info | Preclinical | Severe acute respiratory syndrome (SARS) | [7] | |
| 7 | PMID28216367-compound-6d | Drug Info | Preclinical | Severe acute respiratory syndrome (SARS) | [8] | |
| Drugs in Phase 2 Trial | [+] 1 | + | ||||
| 1 | Lopinavir + ritonavir + interferon beta-1b | Drug Info | Phase 2/3 | Middle East Respiratory Syndrome (MERS) | [3], [4] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 10 Inhibitor drugs | + | ||||
| 1 | Lopinavir + ritonavir + interferon beta-1b | Drug Info | [4] | |||
| 2 | GC376 | Drug Info | [5] | |||
| 3 | GC813 | Drug Info | [1] | |||
| 4 | GRL-001 | Drug Info | [6] | |||
| 5 | Lopinavir | Drug Info | [6] | |||
| 6 | PMID26868298-compound-N3 | Drug Info | [6] | |||
| 7 | PMID27240464-compound-3f | Drug Info | [7] | |||
| 8 | PMID28216367-compound-6d | Drug Info | [8] | |||
| 9 | Lopinavir + ritonavir + interferon beta | Drug Info | [4] | |||
| 10 | Ribavirin + lopinavir + ritonavir + interferon alfa-2a | Drug Info | [4] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| References | Top | |||||
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| REF 1 | Structure-guided Design of Potent and Permeable Inhibitors of MERS Coronavirus 3CL Protease That Utilize a Piperidine Moiety as a Novel Design Element Eur J Med Chem. 2018 Apr 25;150:334-346. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | ClinicalTrials.gov (NCT02845843) MERS-CoV Infection tReated With A Combination of Lopinavir /Ritonavir and Interferon Beta-1b | |||||
| REF 4 | Coronavirus puts drug repurposing on the fast track. Nat Biotechnol. 2020 Apr;38(4):379-381. | |||||
| REF 5 | 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 6 | Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47. | |||||
| REF 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. | |||||
| REF 8 | Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors. Antiviral Res. 2017 May;141:101-106. | |||||
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