Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T31595
|
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| Former ID |
TTDS00174
|
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| Target Name |
Neuraminidase
|
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| Gene Name |
NEU1
|
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| Synonyms |
N-acylneuraminate glycohydrolase; NANase; STNA; Sialidase; NEU1
|
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| Target Type |
Successful
|
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| Disease | Influenza virus [ICD10: J11.1] | ||||
| Function |
Unlike other strains, A/WSN/33 neuraminidase binds and activates plasminogen into plasmin in the vicinity of HA so that activated plasmin cleaves HA rendering the virus infectious.
|
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| BioChemical Class |
Glycosylases
|
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| Target Validation |
T31595
|
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| UniProt ID | |||||
| EC Number |
EC 3.2.1.18
|
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| Sequence |
MTGERPSTALPDRRWGPRILGFWGGCRVWVFAAIFLLLSXAASWSKAENDFGLVQPLVTM
EQLLWVSGRQIGSVDTFRIPLITATPRGTLLAFAEARKMSSSDEGAKFIALRRSMDQ |
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| Drugs and Mode of Action | |||||
| Drug(s) | Oseltamivir | Drug Info | Approved | Influenza virus | [536361] |
| Peramivir | Drug Info | Approved | Influenza virus | [533123] | |
| Zanamivir | Drug Info | Approved | Influenza virus | [536361] | |
| CS-8958 | Drug Info | Phase 3 | Influenza virus | [522510] | |
| DAS-181 | Drug Info | Phase 2 | Influenza virus | [530501] | |
| BCX-140 | Drug Info | Terminated | Influenza virus | [546097] | |
| GS-3435 | Drug Info | Terminated | Influenza virus | [545883] | |
| Inhibitor | (E,E)-1,7-Diphenyl-4,6-heptadien-3-one | Drug Info | [530582] | ||
| (E,E)-5-Hydroxy-1,7-diphenyl-4,6-heptadien-3-one | Drug Info | [530582] | |||
| (S)-1,7-Diphenyl-6(E)-hepten-3-ol | Drug Info | [530582] | |||
| 2,4-Deoxy-4-Guanidino-5-N-Acetyl-Neuraminic Acid | Drug Info | [551391] | |||
| 2-Deoxy-2,3-Dehydro-N-Acetyl-Neuraminic Acid | Drug Info | [551393] | |||
| 4-(Acetylamino)-3-Amino Benzoic Acid | Drug Info | [551393] | |||
| 4-(Acetylamino)-3-Guanidinobenzoic Acid | Drug Info | [551391] | |||
| 4-(ACETYLAMINO)-3-HYDROXY-5-NITROBENZOIC ACID | Drug Info | [551374] | |||
| 4-(ACETYLAMINO)-5-AMINO-3-HYDROXYBENZOIC ACID | Drug Info | [551374] | |||
| 4-Amino-2-Deoxy-2,3-Dehydro-N-Neuraminic Acid | Drug Info | [551391] | |||
| 8-DEOXYGARTANIN | Drug Info | [531095] | |||
| A-192558 | Drug Info | [535937], [536084], [536317] | |||
| A-315675 | Drug Info | [535937], [536084], [536317] | |||
| Alpha-D-Mannose | Drug Info | [551393] | |||
| APIGENIN | Drug Info | [530357] | |||
| BCX-140 | Drug Info | [525973], [550868] | |||
| Bcx-1812 | Drug Info | [551393] | |||
| BCX-1827 | Drug Info | [535937], [536084], [536317] | |||
| BCX-1898 | Drug Info | [535937], [536084], [536317] | |||
| BCX-1923 | Drug Info | [535937], [536084], [536317] | |||
| Beta-D-Mannose | Drug Info | [551393] | |||
| Beta-Sialic Acid | Drug Info | [551393] | |||
| CALOPOCARPIN | Drug Info | [530829] | |||
| Cristacarpin | Drug Info | [530829] | |||
| CS-8958 | Drug Info | [536970] | |||
| CUDRATRICUSXANTHONE | Drug Info | [530017] | |||
| Cudratricusxanthone F | Drug Info | [530017] | |||
| Cudraxanthone D | Drug Info | [530017] | |||
| Cudraxanthone L | Drug Info | [530017] | |||
| Cudraxanthone M | Drug Info | [530017] | |||
| Cyclopentane amide derivatives 1 | Drug Info | [535937], [536084], [536317] | |||
| Cyclopentane amide derivatives 2 | Drug Info | [535937], [536084], [536317] | |||
| Cyclopentane amide derivatives 3 | Drug Info | [535937], [536084], [536317] | |||
| Cyclopentane amide derivatives 4 | Drug Info | [535937], [536084], [536317] | |||
| DANA | Drug Info | [535937], [536084], [536317] | |||
| DAS-181 | Drug Info | [525973], [530501] | |||
| DEMETHYLMEDICARPIN | Drug Info | [530829] | |||
| ERYSTAGALLIN A | Drug Info | [530829] | |||
| Erysubin D | Drug Info | [530829] | |||
| Erysubin E | Drug Info | [530829] | |||
| Erythribyssin D | Drug Info | [530829] | |||
| Erythribyssin L | Drug Info | [530829] | |||
| Erythribyssin M | Drug Info | [530829] | |||
| Erythribyssin O | Drug Info | [530829] | |||
| Eryvarin D | Drug Info | [530829] | |||
| FANA | Drug Info | [535937], [536084], [536317] | |||
| Fucose | Drug Info | [551393] | |||
| Gamma-mangostin | Drug Info | [531095] | |||
| GARCINONE D | Drug Info | [531095] | |||
| GARTANIN | Drug Info | [531095] | |||
| GOSSYPETIN | Drug Info | [530357] | |||
| GS4071 | Drug Info | [535937], [536084], [536317] | |||
| HERBACETIN | Drug Info | [530357] | |||
| ISONEORAUTENOL | Drug Info | [530829] | |||
| KAEMPFEROL | Drug Info | [530357] | |||
| KATSUMADAIN A | Drug Info | [530582] | |||
| Lactose | Drug Info | [551393] | |||
| MACLURAXANTHONE | Drug Info | [530017] | |||
| MANGIFERIN | Drug Info | [530017] | |||
| MANGOSTANIN | Drug Info | [531095] | |||
| MANGOSTANOL | Drug Info | [531095] | |||
| MANGOSTENONE F | Drug Info | [531095] | |||
| MANGOSTENONE G | Drug Info | [531095] | |||
| MANGOSTIN | Drug Info | [531095] | |||
| NEORAUTENOL | Drug Info | [530829] | |||
| O-Sialic Acid | Drug Info | [551374] | |||
| Oseltamivir | Drug Info | [535258], [536654] | |||
| Peramivir | Drug Info | [536654], [536970] | |||
| PHASEOLIN | Drug Info | [530829] | |||
| PHASEOLLIDIN | Drug Info | [530829] | |||
| RHODIOLININ | Drug Info | [530357] | |||
| SMEATHXANTHONE A | Drug Info | [531095] | |||
| Zanamivir | Drug Info | [535258], [536654] | |||
| Modulator | GS-3435 | Drug Info | [525973], [550901] | ||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| DRM | DRM Info | ||||
| Pathways | |||||
| KEGG Pathway | Other glycan degradation | ||||
| References | |||||
| Ref 522510 | ClinicalTrials.gov (NCT00803595) A Multinational Phase III Study of CS-8958 (MARVEL). U.S. National Institutes of Health. | ||||
| Ref 530501 | Inhibition of neuraminidase inhibitor-resistant influenza virus by DAS181, a novel sialidase fusion protein. PLoS One. 2009 Nov 6;4(11):e7838. | ||||
| Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
| Ref 525973 | Neuraminidase inhibitors: zanamivir and oseltamivir. Ann Pharmacother. 2001 Jan;35(1):57-70. | ||||
| Ref 530017 | Bioorg Med Chem. 2009 Apr 1;17(7):2744-50. Epub 2009 Feb 26.Characteristic of neuraminidase inhibitory xanthones from Cudrania tricuspidata. | ||||
| Ref 530357 | Bioorg Med Chem. 2009 Oct 1;17(19):6816-23. Epub 2009 Aug 21.Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities. | ||||
| Ref 530501 | Inhibition of neuraminidase inhibitor-resistant influenza virus by DAS181, a novel sialidase fusion protein. PLoS One. 2009 Nov 6;4(11):e7838. | ||||
| Ref 530582 | J Med Chem. 2010 Jan 28;53(2):778-86.Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai. | ||||
| Ref 530829 | Bioorg Med Chem. 2010 May 1;18(9):3335-44. Epub 2010 Mar 9.Prenylated pterocarpans as bacterial neuraminidase inhibitors. | ||||
| Ref 531095 | Bioorg Med Chem. 2010 Sep 1;18(17):6258-64. Epub 2010 Jul 19.Xanthones with neuraminidase inhibitory activity from the seedcases of Garcinia mangostana. | ||||
| Ref 535258 | Antiviral agents for influenza, hepatitis C and herpesvirus, enterovirus and rhinovirus infections. Med J Aust. 2001 Jul 16;175(2):112-6. | ||||
| Ref 535937 | Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives. J Med Chem. 2004 Apr 8;47(8):1919-29. | ||||
| Ref 536084 | Comparison of the anti-influenza virus activity of cyclopentane derivatives with oseltamivir and zanamivir in vivo. Bioorg Med Chem. 2005 Jun 2;13(12):4071-7. Epub 2005 Apr 25. | ||||
| Ref 536317 | Antiviral agents active against influenza A viruses. Nat Rev Drug Discov. 2006 Dec;5(12):1015-25. | ||||
| Ref 536654 | Current and future antiviral therapy of severe seasonal and avian influenza. Antiviral Res. 2008 Apr;78(1):91-102. Epub 2008 Feb 4. | ||||
| Ref 536970 | Developing new antiviral agents for influenza treatment: what does the future hold? Clin Infect Dis. 2009 Jan 1;48 Suppl 1:S3-13. | ||||
| Ref 550868 | CN patent application no. 104447481, Benzoic acid thiourea anti-influenza virus compounds as well as preparation method and use thereof. | ||||
| Ref 550901 | US patent application no. 2010,0081,713, Compositions and methods for treating viral infections. | ||||
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