Target Information
Target General Infomation | |||||
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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 | [1] |
Peramivir | Drug Info | Approved | Influenza virus | [2] | |
Zanamivir | Drug Info | Approved | Influenza virus | [1] | |
CS-8958 | Drug Info | Phase 3 | Influenza virus | [3] | |
DAS-181 | Drug Info | Phase 2 | Influenza virus | [4] | |
BCX-140 | Drug Info | Terminated | Influenza virus | [5] | |
GS-3435 | Drug Info | Terminated | Influenza virus | [6] | |
Inhibitor | (E,E)-1,7-Diphenyl-4,6-heptadien-3-one | Drug Info | [7] | ||
(E,E)-5-Hydroxy-1,7-diphenyl-4,6-heptadien-3-one | Drug Info | [7] | |||
(S)-1,7-Diphenyl-6(E)-hepten-3-ol | Drug Info | [7] | |||
2,4-Deoxy-4-Guanidino-5-N-Acetyl-Neuraminic Acid | Drug Info | [8] | |||
2-Deoxy-2,3-Dehydro-N-Acetyl-Neuraminic Acid | Drug Info | [9] | |||
4-(Acetylamino)-3-Amino Benzoic Acid | Drug Info | [9] | |||
4-(Acetylamino)-3-Guanidinobenzoic Acid | Drug Info | [8] | |||
4-(ACETYLAMINO)-3-HYDROXY-5-NITROBENZOIC ACID | Drug Info | [10] | |||
4-(ACETYLAMINO)-5-AMINO-3-HYDROXYBENZOIC ACID | Drug Info | [10] | |||
4-Amino-2-Deoxy-2,3-Dehydro-N-Neuraminic Acid | Drug Info | [8] | |||
8-DEOXYGARTANIN | Drug Info | [11] | |||
A-192558 | Drug Info | [12], [13], [14] | |||
A-315675 | Drug Info | [12], [13], [14] | |||
Alpha-D-Mannose | Drug Info | [9] | |||
APIGENIN | Drug Info | [15] | |||
BCX-140 | Drug Info | [16], [17] | |||
Bcx-1812 | Drug Info | [9] | |||
BCX-1827 | Drug Info | [12], [13], [14] | |||
BCX-1898 | Drug Info | [12], [13], [14] | |||
BCX-1923 | Drug Info | [12], [13], [14] | |||
Beta-D-Mannose | Drug Info | [9] | |||
Beta-Sialic Acid | Drug Info | [9] | |||
CALOPOCARPIN | Drug Info | [18] | |||
Cristacarpin | Drug Info | [18] | |||
CS-8958 | Drug Info | [19] | |||
CUDRATRICUSXANTHONE | Drug Info | [20] | |||
Cudratricusxanthone F | Drug Info | [20] | |||
Cudraxanthone D | Drug Info | [20] | |||
Cudraxanthone L | Drug Info | [20] | |||
Cudraxanthone M | Drug Info | [20] | |||
Cyclopentane amide derivatives 1 | Drug Info | [12], [13], [14] | |||
Cyclopentane amide derivatives 2 | Drug Info | [12], [13], [14] | |||
Cyclopentane amide derivatives 3 | Drug Info | [12], [13], [14] | |||
Cyclopentane amide derivatives 4 | Drug Info | [12], [13], [14] | |||
DANA | Drug Info | [12], [13], [14] | |||
DAS-181 | Drug Info | [16], [4] | |||
DEMETHYLMEDICARPIN | Drug Info | [18] | |||
ERYSTAGALLIN A | Drug Info | [18] | |||
Erysubin D | Drug Info | [18] | |||
Erysubin E | Drug Info | [18] | |||
Erythribyssin D | Drug Info | [18] | |||
Erythribyssin L | Drug Info | [18] | |||
Erythribyssin M | Drug Info | [18] | |||
Erythribyssin O | Drug Info | [18] | |||
Eryvarin D | Drug Info | [18] | |||
FANA | Drug Info | [12], [13], [14] | |||
Fucose | Drug Info | [9] | |||
Gamma-mangostin | Drug Info | [11] | |||
GARCINONE D | Drug Info | [11] | |||
GARTANIN | Drug Info | [11] | |||
GOSSYPETIN | Drug Info | [15] | |||
GS4071 | Drug Info | [12], [13], [14] | |||
HERBACETIN | Drug Info | [15] | |||
ISONEORAUTENOL | Drug Info | [18] | |||
KAEMPFEROL | Drug Info | [15] | |||
KATSUMADAIN A | Drug Info | [7] | |||
Lactose | Drug Info | [9] | |||
MACLURAXANTHONE | Drug Info | [20] | |||
MANGIFERIN | Drug Info | [20] | |||
MANGOSTANIN | Drug Info | [11] | |||
MANGOSTANOL | Drug Info | [11] | |||
MANGOSTENONE F | Drug Info | [11] | |||
MANGOSTENONE G | Drug Info | [11] | |||
MANGOSTIN | Drug Info | [11] | |||
NEORAUTENOL | Drug Info | [18] | |||
O-Sialic Acid | Drug Info | [10] | |||
Oseltamivir | Drug Info | [21], [22] | |||
Peramivir | Drug Info | [22], [19] | |||
PHASEOLIN | Drug Info | [18] | |||
PHASEOLLIDIN | Drug Info | [18] | |||
RHODIOLININ | Drug Info | [15] | |||
SMEATHXANTHONE A | Drug Info | [11] | |||
Zanamivir | Drug Info | [21], [22] | |||
Modulator | GS-3435 | Drug Info | [16], [23] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
DRM | DRM Info | ||||
Pathways | |||||
KEGG Pathway | Other glycan degradation | ||||
References | |||||
REF 1 | 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 2 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | ||||
REF 3 | ClinicalTrials.gov (NCT00803595) A Multinational Phase III Study of CS-8958 (MARVEL). U.S. National Institutes of Health. | ||||
REF 4 | Inhibition of neuraminidase inhibitor-resistant influenza virus by DAS181, a novel sialidase fusion protein. PLoS One. 2009 Nov 6;4(11):e7838. | ||||
REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006335) | ||||
REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005196) | ||||
REF 7 | J Med Chem. 2010 Jan 28;53(2):778-86.Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai. | ||||
REF 8 | DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January | ||||
REF 9 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
REF 10 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | ||||
REF 11 | 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 12 | Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives. J Med Chem. 2004 Apr 8;47(8):1919-29. | ||||
REF 13 | 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 14 | Antiviral agents active against influenza A viruses. Nat Rev Drug Discov. 2006 Dec;5(12):1015-25. | ||||
REF 15 | 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 16 | Neuraminidase inhibitors: zanamivir and oseltamivir. Ann Pharmacother. 2001 Jan;35(1):57-70. | ||||
REF 17 | CN patent application no. 104447481, Benzoic acid thiourea anti-influenza virus compounds as well as preparation method and use thereof. | ||||
REF 18 | Bioorg Med Chem. 2010 May 1;18(9):3335-44. Epub 2010 Mar 9.Prenylated pterocarpans as bacterial neuraminidase inhibitors. | ||||
REF 19 | Developing new antiviral agents for influenza treatment: what does the future hold? Clin Infect Dis. 2009 Jan 1;48 Suppl 1:S3-13. | ||||
REF 20 | Bioorg Med Chem. 2009 Apr 1;17(7):2744-50. Epub 2009 Feb 26.Characteristic of neuraminidase inhibitory xanthones from Cudrania tricuspidata. | ||||
REF 21 | Antiviral agents for influenza, hepatitis C and herpesvirus, enterovirus and rhinovirus infections. Med J Aust. 2001 Jul 16;175(2):112-6. | ||||
REF 22 | Current and future antiviral therapy of severe seasonal and avian influenza. Antiviral Res. 2008 Apr;78(1):91-102. Epub 2008 Feb 4. | ||||
REF 23 | US patent application no. 2010,0081,713, Compositions and methods for treating viral infections. |
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