TTD Target ID: TTDS00174

Target Information
Name	Neuraminidase
Type of target	Successful target
Synonyms	N-acylneuraminate glycohydrolase
	NANase
	STNA
	Sialidase
Disease	Influenza, virus not identified    [1]
Drug(s)	Oseltamivir		Approved	Influenza virus infection	[2][3]
	Zanamivir		Approved	Influenza virus infection	[2][3]
	CS-8958		Phase III	Influenza virus infection	[4]
	Peramivir		Phase III	Influenza virus infection	[4][2]
BioChemical Class	Glycosylases
EC Number	EC 3.2.1.18
Pathway	Lysosome
	Other glycan degradation
	Sphingolipid metabolism
UniProt ID	P06818
	P29768
PDB Structure	1DIL; 1DIM; 2SIL; 2SIM; 3SIL.
Function	Cleaves the terminal sialic acid (n-acetyl neuraminic acid) from carbohydrate chains in glycoproteins providing free sialic acid which can be used as carbon and energy sources. Sialidases have been suggested to be pathogenic factors in microbial infection.
Sequence	MNPNQKIITIGSVSLTIATICFLMQIAILVTTVTLHFKQYECSSPPNNQVMPCEPIIIER NITEIVYLTNTTIDKEICPKLVEYRNWSKPQCKITGFAPFSKDNSIRLSAGGGIWVTREP YVSCDPGKCYQFALGQGTTLDNKHSNDTIHDRTPYRTLLMNELGVPFHLGTRQVCIAWSS SSCHDGKAWLHVCVTGYDKNATASFIYDGRLVDSIGSWSKNILRTQESECVCINGTCTVV MTDGSASERADTKILFIEEGKIVHISPLSGSAQHVEECSCYPRYPGVRCVCRDNWKGSNR PVVDINVKDYSIVSSYVCSGLVGDTPRKNDRSSSSYCRNPNNEKGNHGVKGWAFDDGNDV WMGRTISEESRSGYETFKVIGGWSTPNSKLQINRQVIVDSDNRSGYSGIFSVEGKSCINR CFYVELIRGREQETRVWWTSNSIVVFCGTSGTYGTGSWPDGADINLMPI
Related US Patent	6,509,359
	6,518,299
	6,548,476
	6,562,861
	6,593,314
Target Validation	Click to Find Target Validation Information.
QSAR Model	Click to Find Target QSAR Model.
Inhibitor	(E,E)-1,7-Diphenyl-4,6-heptadien-3-one		[5]
	(E,E)-5-Hydroxy-1,7-diphenyl-4,6-heptadien-3-one		[5]
	(S)-1,7-Diphenyl-6		[5]
	2,4-Deoxy-4-Guanidino-5-N-Acetyl-Neuraminic Acid		[6]
	2-Deoxy-2,3-Dehydro-N-Acetyl-Neuraminic Acid		[7]
	4- (ACETYLAMINO)-3-HYDROXY-5-NITROBENZOIC ACID		[8]
	4- (ACETYLAMINO)-5-AMINO-3-HYDROXYBENZOIC ACID		[8]
	4- (Acetylamino)-3-Amino Benzoic Acid		[7]
	4- (Acetylamino)-3-Guanidinobenzoic Acid		[6]
	4-Amino-2-Deoxy-2,3-Dehydro-N-Neuraminic Acid		[6]
	8-DEOXYGARTANIN		[9]
	A-192558		[10][11][12]
	A-315675		[10][11][12]
	APIGENIN		[13]
	Alpha-D-Mannose		[7]
	BCX-1812		[10][11][12]
	BCX-1827		[10][11][12]
	BCX-1898		[10][11][12]
	BCX-1923		[10][11][12]
	Bcx-1812		[7]
	Beta-D-Mannose		[7]
	Beta-Sialic Acid		[7]
	CALOPOCARPIN		[14]
	CS-8958		[4]
	CUDRATRICUSXANTHONE		[15]
	Cudratricusxanthone F		[15]
	Cudraxanthone D		[15]
	Cudraxanthone L		[15]
	Cudraxanthone M		[15]
	Cyclopentane amide derivatives 1		[10][11][12]
	Cyclopentane amide derivatives 2		[10][11][12]
	Cyclopentane amide derivatives 3		[10][11][12]
	Cyclopentane amide derivatives 4		[10][11][12]
	DANA		[10][11][12]
	DEMETHYLMEDICARPIN		[14]
	ERYSTAGALLIN A		[14]
	Erythribyssin D		[14]
	Erythribyssin L		[14]
	Erythribyssin M		[14]
	Erythribyssin O		[14]
	FANA		[10][11][12]
	Fucose		[7]
	GARCINONE D		[9]
	GARTANIN		[9]
	GOSSYPETIN		[13]
	GS4071		[10][11][12]
	HERBACETIN		[13]
	ISONEORAUTENOL		[14]
	KAEMPFEROL		[13]
	KATSUMADAIN A		[5]
	Lactose		[7]
	MACLURAXANTHONE		[15]
	MANGIFERIN		[15]
	MANGOSTANIN		[9]
	MANGOSTANOL		[9]
	MANGOSTENONE F		[9]
	MANGOSTENONE G		[9]
	MANGOSTIN		[9]
	NEORAUTENOL		[14]
	O-Sialic Acid		[8]
	OSELTAMIVIR ACID		[16]
	Oseltamivir		[2][3]
	PHASEOLIN		[14]
	PHASEOLLIDIN		[14]
Peramivir		[4][2]
RHODIOLININ		[13]
SMEATHXANTHONE A		[9]
Zanamivir		[2][3]
cristacarpin		[14]
erysubin D		[14]
erysubin E		[14]
eryvarin D		[14]
gamma-mangostin		[9]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
Ref 1	New millennium antivirals against pandemic and epidemic influenza: the neuraminidase inhibitors. Antivir Chem Chemother. 2002 Jul;13(4):205-17. To Reference
Ref 2	Current and future antiviral therapy of severe seasonal and avian influenza. Antiviral Res. 2008 Apr;78(1):91-102. Epub 2008 Feb 4. To Reference
Ref 3	Antiviral agents for influenza, hepatitis C and herpesvirus, enterovirus and rhinovirus infections. Med J Aust. 2001 Jul 16;175(2):112-6. To Reference
Ref 4	Developing new antiviral agents for influenza treatment: what does the future hold? Clin Infect Dis. 2009 Jan 1;48 Suppl 1:S3-13. To Reference
Ref 5	J Med Chem. 2010 Jan 28;53(2):778-86.Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai. To Reference
Ref 6	Nucleic Acids Res. 2011 January; 39(Database issue): D1035¨CD1041. DrugBank 3.0: a comprehensive resource for ¡®Omics¡¯ research on drugs To Reference
Ref 7	Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 8	Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 9	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. To Reference
Ref 10	Antiviral agents active against influenza A viruses. Nat Rev Drug Discov. 2006 Dec;5(12):1015-25. To Reference
Ref 11	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. To Reference
Ref 12	Syntheses and neuraminidase inhibitory activity of multisubstituted cyclopentane amide derivatives. J Med Chem. 2004 Apr 8;47(8):1919-29. To Reference
Ref 13	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. To Reference
Ref 14	Bioorg Med Chem. 2010 May 1;18(9):3335-44. Epub 2010 Mar 9.Prenylated pterocarpans as bacterial neuraminidase inhibitors. To Reference
Ref 15	Bioorg Med Chem. 2009 Apr 1;17(7):2744-50. Epub 2009 Feb 26.Characteristic of neuraminidase inhibitory xanthones from Cudrania tricuspidata. To Reference
Ref 16	Antimicrob Agents Chemother. 2008 Oct;52(10):3484-91. Epub 2008 Aug 11.Limited inhibitory effects of oseltamivir and zanamivir on human sialidases. To Reference

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