Target Information
| Target General Infomation | Top | ||||
|---|---|---|---|---|---|
| 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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| Target Status |
Target in Phase 2 Trial
|
[1] | |||
| Disease | [+] 1 Target-related Diseases | + | |||
| 1 | Middle East Respiratory Syndrome [ICD-11: 1D64] | ||||
| 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 |
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| Drugs and Modes of Action | Top | ||||
|---|---|---|---|---|---|
| Drugs in Phase 2 Trial | [+] 1 Drugs in Phase 2 Trial | + | |||
| 1 | Lopinavir + ritonavir + interferon beta-1b | Drug Info | Phase 2 Trial | MERS | [2], [3] |
| Preclinical Drugs | [+] 7 Preclinical Drugs | + | |||
| 1 | Lopinavir | Drug Info | Preclinical | MERS | [4] |
| 2 | PMID28216367-compound-6d | Drug Info | Preclinical | MERS | [5] |
| 3 | PMID26868298-compound-N3 | Drug Info | Preclinical | MERS | [4] |
| 4 | GC376 | Drug Info | Preclinical | MERS | [6] |
| 5 | PMID27240464-compound-3f | Drug Info | Preclinical | MERS | [7] |
| 6 | GC813 | Drug Info | Preclinical | MERS | [1] |
| 7 | GRL-001 | Drug Info | Preclinical | MERS | [4] |
| Investigative agents | [+] 2 Investigative agents | + | |||
| 1 | Lopinavir + ritonavir + interferon beta | Drug Info | Investigative | MERS | [3], [8] |
| 2 | Ribavirin + lopinavir + ritonavir + interferon alfa-2a | Drug Info | Investigative | MERS | [4], [9] |
| Mode of Action | [+] 1 Modes of Action | + | |||
| Inhibitor | [+] 10 Inhibitor drugs | + | |||
| 1 | Lopinavir + ritonavir + interferon beta-1b | Drug Info | [3] | ||
| 2 | GC376 | Drug Info | [6] | ||
| 3 | GC813 | Drug Info | [1] | ||
| 4 | GRL-001 | Drug Info | [4] | ||
| 5 | Lopinavir | Drug Info | [4] | ||
| 6 | PMID26868298-compound-N3 | Drug Info | [4] | ||
| 7 | PMID27240464-compound-3f | Drug Info | [7] | ||
| 8 | PMID28216367-compound-6d | Drug Info | [5] | ||
| 9 | Lopinavir + ritonavir + interferon beta | Drug Info | [3] | ||
| 10 | Ribavirin + lopinavir + ritonavir + interferon alfa-2a | Drug Info | [3] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| 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. | ||||
| 2 | ClinicalTrials.gov (NCT02845843) MERS-CoV Infection tReated With A Combination of Lopinavir /Ritonavir and Interferon Beta-1b | ||||
| 3 | Coronavirus puts drug repurposing on the fast track. Nat Biotechnol. 2020 Apr;38(4):379-381. | ||||
| 4 | Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47. | ||||
| 5 | Identification and evaluation of potent Middle East respiratory syndrome coronavirus (MERS-CoV) 3CLPro inhibitors. Antiviral Res. 2017 May;141:101-106. | ||||
| 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. | ||||
| 8 | Comparative therapeutic efficacy of remdesivir and combination lopinavir, ritonavir, and interferon beta against MERS-CoV. Nat Commun. 2020 Jan 10;11(1):222. | ||||
| 9 | Therapeutic options for the 2019 novel coronavirus (2019-nCoV). Nat Rev Drug Discov. 2020 Mar;19(3):149-150. | ||||
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