Target Information
| Target General Information | Top | |||||
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| Target ID |
T88595
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| Target Name |
MERS-CoV spike glycoprotein (S)
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| Synonyms |
MERS-CoV S glycoprotein; MERS-CoV E2; MERS-CoV Peplomer protein
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| Gene Name |
MERS-CoV S
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| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | COVID-19 [ICD-11: 1D6Y] | |||||
| Function |
Mediates fusion of the virion and cellular membranes by acting as a class I viral fusion protein. Under the current model, the protein has at least three conformational states: pre-fusion native state, pre-hairpin intermediate state, and post-fusion hairpin state. During viral and target cell membrane fusion, the coiled coil regions (heptad repeats) assume a trimer-of-hairpins structure, positioning the fusion peptide in close proximity to the C-terminal region of the ectodomain. The formation of this structure appears to drive apposition and subsequent fusion of viral and target cell membranes.
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| BioChemical Class |
Betacoronaviruses spike protein family
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| UniProt ID | ||||||
| Sequence |
MIHSVFLLMFLLTPTESYVDVGPDSVKSACIEVDIQQTFFDKTWPRPIDVSKADGIIYPQ
GRTYSNITITYQGLFPYQGDHGDMYVYSAGHATGTTPQKLFVANYSQDVKQFANGFVVRI GAAANSTGTVIISPSTSATIRKIYPAFMLGSSVGNFSDGKMGRFFNHTLVLLPDGCGTLL RAFYCILEPRSGNHCPAGNSYTSFATYHTPATDCSDGNYNRNASLNSFKEYFNLRNCTFM YTYNITEDEILEWFGITQTAQGVHLFSSRYVDLYGGNMFQFATLPVYDTIKYYSIIPHSI RSIQSDRKAWAAFYVYKLQPLTFLLDFSVDGYIRRAIDCGFNDLSQLHCSYESFDVESGV YSVSSFEAKPSGSVVEQAEGVECDFSPLLSGTPPQVYNFKRLVFTNCNYNLTKLLSLFSV NDFTCSQISPAAIASNCYSSLILDYFSYPLSMKSDLSVSSAGPISQFNYKQSFSNPTCLI LATVPHNLTTITKPLKYSYINKCSRLLSDDRTEVPQLVNANQYSPCVSTVPSTVWEDGDY YRKQLSPLEGGGWLVASGSTVAMTEQLQMGFGITVQYGTDTNSVCPKLEFANDTKIASQL GNCVEYSLYGVSGRGVFQNCTAVGVRQQRFVYDAYQNLVGYYSDDGNYYCLRACVSVPVS VIYDKETKTHATLFGSVACEHISSTMSQYSRSTRSMLKRRDSTYGPLQTPVGCVLGLVNS SLFVEDCKLPLGQSLCALPDTPSTLTPRSVRSVPGEMRLASIAFNHPIQVDQLNSSYFKL SIPTNFSFGVTQEYIQTTIQKVTVDCKQYVCNGFQKCEQLLREYGQFCSKINQALHGANL RQDDSVRNLFASVKSSQSSPIIPGFGGDFNLTLLEPVSISTGSRSARSAIEDLLFDKVTI ADPGYMQGYDDCMQQGPASARDLICAQYVAGYKVLPPLMDVNMEAAYTSSLLGSIAGVGW TAGLSSFAAIPFAQSIFYRLNGVGITQQVLSENQKLIANKFNQALGAMQTGFTTTNEAFR KVQDAVNNNAQALSKLASELSNTFGAISASIGDIIQRLDVLEQDAQIDRLINGRLTTLNA FVAQQLVRSESAALSAQLAKDKVNECVKAQSKRSGFCGQGTHIVSFVVNAPNGLYFMHVG YYPSNHIEVVSAYGLCDAANPTNCIAPVNGYFIKTNNTRIVDEWSYTGSSFYAPEPITSL NTKYVAPQVTYQNISTNLPPPLLGNSTGIDFQDELDEFFKNVSTSIPNFGSLTQINTTLL DLTYEMLSLQQVVKALNESYIDLKELGNYTYYNKWPWYIWLGFIAGLVALALCVFFILCC TGCGTNCMGKLKCNRCCDRYEEYDLEPHKVHVH Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Drugs in Phase 2 Trial | [+] 1 | + | ||||
| 1 | Nafamostat | Drug Info | Phase 2/3 | Coronavirus Disease 2019 (COVID-19) | [2] | |
| Discontinued Drugs | [+] 2 | + | ||||
| 1 | REGN 3048 | Drug Info | Discontinued in Phase 1 | Middle East Respiratory Syndrome (MERS) | [3] | |
| 2 | REGN 3051 | Drug Info | Discontinued in Phase 1 | Middle East Respiratory Syndrome (MERS) | [3] | |
| Preclinical Drugs | [+] 7 | + | ||||
| 1 | Alpha-Helical lipopeptides FFS | Drug Info | Preclinical | Middle East Respiratory Syndrome (MERS) | [4] | |
| 2 | Alpha-Helical lipopeptides IIK | Drug Info | Preclinical | Middle East Respiratory Syndrome (MERS) | [4] | |
| 3 | Alpha-Helical lipopeptides IIS | Drug Info | Preclinical | Middle East Respiratory Syndrome (MERS) | [4] | |
| 4 | Alpha-Helical lipopeptides LLS | Drug Info | Preclinical | Middle East Respiratory Syndrome (MERS) | [4] | |
| 5 | MERS-five-helix bundle | Drug Info | Preclinical | Middle East Respiratory Syndrome (MERS) | [5] | |
| 6 | Peptide P21S10 | Drug Info | Preclinical | Middle East Respiratory Syndrome (MERS) | [6] | |
| 7 | PMID26911565-peptide-P9 | Drug Info | Preclinical | Severe acute respiratory syndrome (SARS) | [7] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 10 Inhibitor drugs | + | ||||
| 1 | Nafamostat | Drug Info | [1] | |||
| 2 | REGN 3048 | Drug Info | [8] | |||
| 3 | REGN 3051 | Drug Info | [8] | |||
| 4 | Alpha-Helical lipopeptides FFS | Drug Info | [4] | |||
| 5 | Alpha-Helical lipopeptides IIK | Drug Info | [4] | |||
| 6 | Alpha-Helical lipopeptides IIS | Drug Info | [4] | |||
| 7 | Alpha-Helical lipopeptides LLS | Drug Info | [4] | |||
| 8 | MERS-five-helix bundle | Drug Info | [5] | |||
| 9 | Peptide P21S10 | Drug Info | [6] | |||
| 10 | PMID26911565-peptide-P9 | Drug Info | [7] | |||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| References | Top | |||||
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| REF 1 | Identification of Nafamostat as a Potent Inhibitor of Middle East Respiratory Syndrome Coronavirus S Protein-Mediated Membrane Fusion Using the Split-Protein-Based Cell-Cell Fusion Assay Antimicrob Agents Chemother. 2016 Oct 21;60(11):6532-6539. | |||||
| REF 2 | ClinicalTrials.gov (NCT04352400) Efficacy of Nafamostat in Covid-19 Patients (RACONA Study). U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT03301090) A Safety, Tolerability, Pharmacokinetics and Immunogenicity Trial of Co-administered MERS-CoV Antibodies REGN3048 and REGN3051. U.S. National Institutes of Health. | |||||
| REF 4 | De Novo Design of -Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery. J Med Chem. 2018 Oct 11;61(19):8734-8745. | |||||
| REF 5 | Identification of a Novel Inhibitor against Middle East Respiratory Syndrome Coronavirus. Viruses. 2017 Sep 14;9(9). pii: E255. | |||||
| REF 6 | Discovery of Hydrocarbon-Stapled Short -Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors. J Med Chem. 2018 Mar 8;61(5):2018-2026. | |||||
| REF 7 | A novel peptide with potent and broad-spectrum antiviral activities against multiple respiratory viruses. Sci Rep. 2016 Feb 25;6:22008. | |||||
| REF 8 | Pre- And Postexposure Efficacy of Fully Human Antibodies Against Spike Protein in a Novel Humanized Mouse Model of MERS-CoV Infection. Proc Natl Acad Sci U S A. 2015 Jul 14;112(28):8738-43. doi: 10.1073/pnas.1510830112. | |||||
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