Target General Infomation
Target ID
T31595
Former ID
TTDS00174
Target Name
Neuraminidase
Gene Name
NEU1
Synonyms
N-acylneuraminate glycohydrolase; NANase; STNA; Sialidase; NEU1
Target Type
Successful
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.
BioChemical Class
Glycosylases
Target Validation
T31595
UniProt ID
EC Number
EC 3.2.1.18
Sequence
MTGERPSTALPDRRWGPRILGFWGGCRVWVFAAIFLLLSXAASWSKAENDFGLVQPLVTM
EQLLWVSGRQIGSVDTFRIPLITATPRGTLLAFAEARKMSSSDEGAKFIALRRSMDQ
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 1Natural 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 22014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
REF 3ClinicalTrials.gov (NCT00803595) A Multinational Phase III Study of CS-8958 (MARVEL). U.S. National Institutes of Health.
REF 4Inhibition of neuraminidase inhibitor-resistant influenza virus by DAS181, a novel sialidase fusion protein. PLoS One. 2009 Nov 6;4(11):e7838.
REF 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006335)
REF 6Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005196)
REF 7J Med Chem. 2010 Jan 28;53(2):778-86.Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
REF 8DrugBank 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 9How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 10The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 11Bioorg 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 12Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives. J Med Chem. 2004 Apr 8;47(8):1919-29.
REF 13Comparison 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 14Antiviral agents active against influenza A viruses. Nat Rev Drug Discov. 2006 Dec;5(12):1015-25.
REF 15Bioorg 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 16Neuraminidase inhibitors: zanamivir and oseltamivir. Ann Pharmacother. 2001 Jan;35(1):57-70.
REF 17CN patent application no. 104447481, Benzoic acid thiourea anti-influenza virus compounds as well as preparation method and use thereof.
REF 18Bioorg Med Chem. 2010 May 1;18(9):3335-44. Epub 2010 Mar 9.Prenylated pterocarpans as bacterial neuraminidase inhibitors.
REF 19Developing new antiviral agents for influenza treatment: what does the future hold? Clin Infect Dis. 2009 Jan 1;48 Suppl 1:S3-13.
REF 20Bioorg Med Chem. 2009 Apr 1;17(7):2744-50. Epub 2009 Feb 26.Characteristic of neuraminidase inhibitory xanthones from Cudrania tricuspidata.
REF 21Antiviral agents for influenza, hepatitis C and herpesvirus, enterovirus and rhinovirus infections. Med J Aust. 2001 Jul 16;175(2):112-6.
REF 22Current and future antiviral therapy of severe seasonal and avian influenza. Antiviral Res. 2008 Apr;78(1):91-102. Epub 2008 Feb 4.
REF 23US patent application no. 2010,0081,713, Compositions and methods for treating viral infections.

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