Target Information
| Target General Information | Top | |||||
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| Target ID |
T87374
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| Target Name |
COVID-19 spike glycoprotein (S)
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| Synonyms |
COVID-19 S glycoprotein; COVID-19 E2; COVID-19 Peplomer protein
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| Gene Name |
COVID-19 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 | ||||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | GSK4182136 | Drug Info | Approved in EU | Coronavirus Disease 2019 (COVID-19) | [2] | |
| Clinical Trial Drug(s) | [+] 6 Clinical Trial Drugs | + | ||||
| 1 | LY-CoV555 | Drug Info | Phase 3 | Coronavirus Disease 2019 (COVID-19) | [3] | |
| 2 | REGN-COV2 | Drug Info | Phase 2 | Coronavirus Disease 2019 (COVID-19) | [5] | |
| 3 | JS016 | Drug Info | Phase 1/2 | Coronavirus Disease 2019 (COVID-19) | [6] | |
| 4 | GSK4182137 | Drug Info | Phase 1 | Coronavirus Disease 2019 (COVID-19) | [2] | |
| 5 | REGN3048 | Drug Info | Phase 1 | Coronavirus infection | [7] | |
| 6 | REGN3051 | Drug Info | Phase 1 | Coronavirus infection | [7] | |
| Drugs in Phase 2 Trial | [+] 1 | + | ||||
| 1 | Nafamostat | Drug Info | Phase 2/3 | Coronavirus Disease 2019 (COVID-19) | [4] | |
| Preclinical Drug(s) | [+] 3 Preclinical Drugs | + | ||||
| 1 | m337 | Drug Info | Preclinical | Coronavirus infection | [8] | |
| 2 | MERS-27 | Drug Info | Preclinical | Coronavirus infection | [8] | |
| 3 | MERS-4 | Drug Info | Preclinical | Coronavirus infection | [8] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 10 Inhibitor drugs | + | ||||
| 1 | LY-CoV555 | Drug Info | [9] | |||
| 2 | Nafamostat | Drug Info | [1] | |||
| 3 | REGN-COV2 | Drug Info | [10] | |||
| 4 | JS016 | Drug Info | [11] | |||
| 5 | REGN3048 | Drug Info | [12] | |||
| 6 | REGN3051 | Drug Info | [12] | |||
| 7 | m337 | Drug Info | [8] | |||
| 8 | MERS-27 | Drug Info | [8] | |||
| 9 | MERS-4 | Drug Info | [8] | |||
| 10 | Toremifene | Drug Info | [13] | |||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Tretinoin | Ligand Info | |||||
| Structure Description | Cryo-EM structure of the SARS-CoV-2 spike glycoprotein in complex with all-trans retinoic acid | PDB:7Y42 | ||||
| Method | Electron microscopy | Resolution | 3.45 Å | Mutation | Yes | [14] |
| PDB Sequence |
AYTNSFTRGV
36 YYPDKVFRSS46 VLHSTQDLFL56 PFFSNVTWFH66 AIHVGVYFAS94 SNIIRGWIFG 107 TTLDSKTQSL117 LIVNNATNVV127 IKVCFTFEYV171 SQKNLREFVF194 FKIYSKHTPD 215 LPQGFSALEV227 DLPIGINIAY265 YVGYLQPRTF275 LLKYNENGTI285 TDAVDCALDP 295 LSETKCTLKS305 FTVEKGIYQT315 SNTESIVRFP330 NITNLCPFGE340 VFNATRFASV 350 YAWNRKRISN360 CVADYSVLYN370 SASFSTFKCY380 GVSPTKLNDL390 CFTNVYADSF 400 VIRGDEVRQI410 APGQTGKIAD420 YNYKLPDDFT430 GCVIAWNSNN440 LDSKGNYNYL 452 YRLFRKSNLK462 PFERDISTEI472 YQAGSTPCNG482 VEGFNCYFPL492 QSYGFQPTNG 502 VGYQPYRVVV512 LSFELLHAPA522 TVCGPKKSTN532 LVKNKCVNFN542 FNGLTGTGVL 552 TESNKKFLPF562 QQFGRDIADT572 TDAVRDPQTL582 EILDITPCSF592 GGVSVITPGT 602 NTSNQVAVLY612 QDVNCTEVPD627 QLTPTWRVYS637 TGSNVFQTRA647 GCLIGAEHVN 657 NSYECDIPIG667 AGICASYQTS689 QSIIAYTMSL699 GAENSVAYSN709 NSIAIPTNFT 719 ISVTTEILPV729 SMTKTSVDCT739 MYICGDSTEC749 SNLLLQYGSF759 CTQLNRALTG 769 IAVEQDKNTQ779 EVFAQVKQIY789 KTPPIKDFGG799 FNFSQILPDP809 SKPSKRSFIE 819 DLLFNKVTDL849 ICAQKFNGLT859 VLPPLLTDEM869 IAQYTSALLA879 GTITSGWTFG 889 AGAALQIPFA899 MQMAYRFNGI909 GVTQNVLYEN919 QKLIANQFNS929 AIGKIQDSLS 939 STASALGKLQ949 DVVNQNAQAL959 NTLVKQLSSN969 FGAISSVLND979 ILSRLDPPEA 989 EVQIDRLITG999 RLQSLQTYVT1009 QQLIRAAEIR1019 ASANLAATKM1029 SECVLGQSKR 1039 VDFCGKGYHL1049 MSFPQSAPHG1059 VVFLHVTYVP1069 AQEKNFTTAP1079 AICHDGKAHF 1089 PREGVFVSNG1099 THWFVTQRNF1109 YEPQIITTDN1119 TFVSGNCDVV1129 IGIVNNTVYD 1139 PLQPELDS
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| Ligand Name: Linoleic acid | Ligand Info | |||||
| Structure Description | SARS-CoV-2 Spike with ethylbenzamide-tri-iodo Siallyllactose, C3 symmetry | PDB:7QUR | ||||
| Method | Electron microscopy | Resolution | 2.27 Å | Mutation | Yes | [15] |
| PDB Sequence |
QCVNLTTRTQ
23 LPPAYTNSFT33 RGVYYPDKVF43 RSSVLHSTQD53 LFLPFFSNVT63 WFHAIHVSGT 73 NGTKRFDNPV83 LPFNDGVYFA93 STEKSNIIRG103 WIFGTTLDSK113 TQSLLIVNNA 123 TNVVIKVCEF133 QFCNDPFLGV143 YYHKNNKSWM153 ESEFRVYSSA163 NNCTFEYVSQ 173 PFLMDLEGKQ183 GNFKNLREFV193 FKNIDGYFKI203 YSKHTPINLV213 RDLPQGFSAL 223 EPLVDLPIGI233 NITRFQTLLA243 LHRSYLTPGD253 SSSGWTAGAA263 AYYVGYLQPR 273 TFLLKYNENG283 TITDAVDCAL293 DPLSETKCTL303 KSFTVEKGIY313 QTSNFRVQPT 323 ESIVRFPNIT333 NLCPFGEVFN343 ATRFASVYAW353 NRKRISNCVA363 DYSVLYNSAS 373 FSTFKCYGVS383 PTKLNDLCFT393 NVYADSFVIR403 GDEVRQIAPG413 QTGKIADYNY 423 KLPDDFTGCV433 IAWNSNNLDS443 KVGGNYNYLY453 RLFRKSNLKP463 FERDISTEIY 473 QAGSTPCNGV483 EGFNCYFPLQ493 SYGFQPTNGV503 GYQPYRVVVL513 SFELLHAPAT 523 VCGPKKSTNL533 VKNKCVNFNF543 NGLTGTGVLT553 ESNKKFLPFQ563 QFGRDIADTT 573 DAVRDPQTLE583 ILDITPCSFG593 GVSVITPGTN603 TSNQVAVLYQ613 DVNCTTWRVY 636 STGSNVFQTR646 AGCLIGAEHV656 NNSYECDIPI666 GAGICASYQT676 SQSIIAYTMS 698 LGAENSVAYS708 NNSIAIPTNF718 TISVTTEILP728 VSMTKTSVDC738 TMYICGDSTE 748 CSNLLLQYGS758 FCTQLNRALT768 GIAVEQDKNT778 QEVFAQVKQI788 YKTPPIKDFG 798 GFNFSQILPD808 PSKPSKRSFI818 EDLLFNKVTL828 ADAGFIKQYG838 DCLGDIAARD 848 LICAQKFNGL858 TVLPPLLTDE868 MIAQYTSALL878 AGTITSGWTF888 GAGAALQIPF 898 AMQMAYRFNG908 IGVTQNVLYE918 NQKLIANQFN928 SAIGKIQDSL938 SSTASALGKL 948 QDVVNQNAQA958 LNTLVKQLSS968 NFGAISSVLN978 DILSRLDKVE988 AEVQIDRLIT 998 GRLQSLQTYV1008 TQQLIRAAEI1018 RASANLAATK1028 MSECVLGQSK1038 RVDFCGKGYH 1048 LMSFPQSAPH1058 GVVFLHVTYV1068 PAQEKNFTTA1078 PAICHDGKAH1088 FPREGVFVSN 1098 GTHWFVTQRN1108 FYEPQIITTD1118 NTFVSGNCDV1128 VIGIVNNTVY1138 D |
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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There is no similarity protein (E value < 0.005) for this target
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| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| References | Top | |||||
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| REF 1 | Therapeutic options for the 2019 novel coronavirus (2019-nCoV). Nat Rev Drug Discov. 2020 Mar;19(3):149-150. | |||||
| REF 2 | Clinical pipeline report, company report or official report of GlaxoSmithKline | |||||
| REF 3 | ClinicalTrials.gov (NCT04497987) A Study of LY3819253 (LY-CoV555) and LY3832479 (LY-CoV016) in Preventing SARS-CoV-2 Infection and COVID-19 in Nursing Home Residents and Staff (BLAZE-2). U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT04352400) Efficacy of Nafamostat in Covid-19 Patients (RACONA Study). U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT04852978) COVID-19 Study to Assess Immunogenicity, Safety, and Tolerability of Moderna mRNA-1273 Vaccine Administered With Casirivimab+Imdevimab in Healthy Adult Volunteers. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT04780321) JS016 (Anti-SARS-CoV-2 Monoclonal Antibody)With Mild and Moderate COVID-19 or SARS-CoV-2 Asymptomatic Infection Subects. U.S. National Institutes of Health. | |||||
| REF 7 | 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 8 | Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47. | |||||
| REF 9 | Neutralizing Antibody LY-CoV555 for Outpatient Covid-19. Reply. N Engl J Med. 2021 Jan 14;384(2):189. | |||||
| REF 10 | REGN-COV2, a Neutralizing Antibody Cocktail, in Outpatients with Covid-19. N Engl J Med. 2021 Jan 21;384(3):238-251. | |||||
| REF 11 | Clinical pipeline report, company report or official report of Lilly. | |||||
| REF 12 | Prophylactic and therapeutic efficacy of mAb treatment against MERS-CoV in common marmosets. Antiviral Res. 2018 Aug;156:64-71. | |||||
| REF 13 | Repurposing of FDA-Approved Toremifene to Treat COVID-19 by Blocking the Spike Glycoprotein and NSP14 of SARS-CoV-2. June 5, 2020. | |||||
| REF 14 | A Retinol Derivative Inhibits SARS-CoV-2 Infection by Interrupting Spike-Mediated Cellular Entry. mBio. 2022 Aug 30;13(4):e0148522. | |||||
| REF 15 | Pathogen-sugar interactions revealed by universal saturation transfer analysis. Science. 2022 Jul 22;377(6604):eabm3125. | |||||
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