Target Information

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
Q6Q4G9
EC Number
EC 3.2.1.18
Sequence
MTGERPSTALPDRRWGPRILGFWGGCRVWVFAAIFLLLSXAASWSKAENDFGLVQPLVTM
EQLLWVSGRQIGSVDTFRIPLITATPRGTLLAFAEARKMSSSDEGAKFIALRRSMDQ
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 522510ClinicalTrials.gov (NCT00803595) A Multinational Phase III Study of CS-8958 (MARVEL). U.S. National Institutes of Health.
Ref 530501Inhibition of neuraminidase inhibitor-resistant influenza virus by DAS181, a novel sialidase fusion protein. PLoS One. 2009 Nov 6;4(11):e7838.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 536361Natural 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 545883Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005196)
Ref 546097Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006335)
Ref 525973Neuraminidase inhibitors: zanamivir and oseltamivir. Ann Pharmacother. 2001 Jan;35(1):57-70.
Ref 530017Bioorg Med Chem. 2009 Apr 1;17(7):2744-50. Epub 2009 Feb 26.Characteristic of neuraminidase inhibitory xanthones from Cudrania tricuspidata.
Ref 530357Bioorg 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 530501Inhibition of neuraminidase inhibitor-resistant influenza virus by DAS181, a novel sialidase fusion protein. PLoS One. 2009 Nov 6;4(11):e7838.
Ref 530582J Med Chem. 2010 Jan 28;53(2):778-86.Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
Ref 530829Bioorg Med Chem. 2010 May 1;18(9):3335-44. Epub 2010 Mar 9.Prenylated pterocarpans as bacterial neuraminidase inhibitors.
Ref 531095Bioorg 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 535258Antiviral agents for influenza, hepatitis C and herpesvirus, enterovirus and rhinovirus infections. Med J Aust. 2001 Jul 16;175(2):112-6.
Ref 535937Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives. J Med Chem. 2004 Apr 8;47(8):1919-29.
Ref 536084Comparison 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 536317Antiviral agents active against influenza A viruses. Nat Rev Drug Discov. 2006 Dec;5(12):1015-25.
Ref 536654Current and future antiviral therapy of severe seasonal and avian influenza. Antiviral Res. 2008 Apr;78(1):91-102. Epub 2008 Feb 4.
Ref 536970Developing new antiviral agents for influenza treatment: what does the future hold? Clin Infect Dis. 2009 Jan 1;48 Suppl 1:S3-13.
Ref 550868CN patent application no. 104447481, Benzoic acid thiourea anti-influenza virus compounds as well as preparation method and use thereof.
Ref 550901US patent application no. 2010,0081,713, Compositions and methods for treating viral infections.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551391DrugBank 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 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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