Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T31595 | ||||
Target Name | Neuraminidase | ||||
Target Type | Successful |
||||
Drug Potency against Target | Peramivir | Drug Info | IC50 = 1.8 nM | [552600] | |
GOSSYPETIN | Drug Info | IC50 = 800 nM | [530357] | ||
(E,E)-5-Hydroxy-1,7-diphenyl-4,6-heptadien-3-one | Drug Info | IC50 = 4670 nM | [530582] | ||
(S)-1,7-Diphenyl-6(E)-hepten-3-ol | Drug Info | IC50 = 4130 nM | [530582] | ||
Cudraxanthone M | Drug Info | IC50 = 186 nM | [530017] | ||
(E,E)-1,7-Diphenyl-4,6-heptadien-3-one | Drug Info | IC50 = 6100 nM | [530582] | ||
Zanamivir | Drug Info | IC50 = 1.8 nM | [552600] | ||
HERBACETIN | Drug Info | IC50 = 1400 nM | [530357] | ||
KAEMPFEROL | Drug Info | IC50 = 8000 nM | [530357] | ||
MANGOSTENONE G | Drug Info | Ki = 6800 nM | [531095] | ||
8-DEOXYGARTANIN | Drug Info | Ki = 15500 nM | [531095] | ||
MANGOSTENONE F | Drug Info | Ki = 7600 nM | [531095] | ||
SMEATHXANTHONE A | Drug Info | Ki = 150 nM | [531095] | ||
CUDRATRICUSXANTHONE | Drug Info | IC50 = 245 nM | [530017] | ||
MANGOSTIN | Drug Info | Ki = 5800 nM | [531095] | ||
MANGOSTANOL | Drug Info | Ki = 6500 nM | [531095] | ||
Cudraxanthone D | Drug Info | IC50 = 278 nM | [530017] | ||
MANGIFERIN | Drug Info | IC50 = 16200 nM | [530017] | ||
GARTANIN | Drug Info | Ki = 3600 nM | [531095] | ||
KATSUMADAIN A | Drug Info | IC50 = 1050 nM | [530582] | ||
MACLURAXANTHONE | Drug Info | IC50 = 186 nM | [530017] | ||
RHODIOLININ | Drug Info | IC50 = 6100 nM | [530357] | ||
APIGENIN | Drug Info | IC50 = 17400 nM | [530357] | ||
Cudraxanthone L | Drug Info | IC50 = 228 nM | [530017] | ||
Gamma-mangostin | Drug Info | Ki = 800 nM | [531095] | ||
MANGOSTANIN | Drug Info | Ki = 5900 nM | [531095] | ||
GARCINONE D | Drug Info | Ki = 3300 nM | [531095] | ||
Action against Disease Model | Oseltamivir | Influenza virus neuraminidase inhibitors (NAIs) were introduced in clinical practice in various parts of the world since 1999 but were only scarcely distributed in France. Priorto the generalization of zanamivir and oseltamivir utilization in our country, we decided to test a large panel of influenza strains to establish the baseline sensitivity of these viruses to anti-neuraminidase drugs, based upon a fluorometric neuraminidase enzymatic test. Our study was performed on clinical samples collected by practitioners of the GROG network (Groupe R?|gional d'Observation de la Grippe) in the south of France during the 2002-2003 influenza season. Out of 355 isolates tested in the fluorometric neuraminidase activity assay, 267 isolates could be included in inhibition assayagainst anti-neuraminidase drugs. Differences in IC50 range were found according to the subtype and the anti-neuraminidase drug. Influenza B and A/H1N1 viruses appeared to be more sensitive to zanamivir than to oseltamivir (mean B IC50 values: 4.19 nM versus 13 nM; mean H1N1 IC50 values: 0.92 nM versus 1.34 nM), while A/H1N2 and A/H3N2 viruses were more sensitive to oseltamivir than to zanamivir (mean H3N2 IC50 values: 0.67 nM versus 2.28 nM; mean H1N2 IC50 values: 0.9 nM versus 3.09 nM). Out of 128 N2 carrying isolates, 10 isolates had zanamivir or oseltamivir IC50 values in upper limits compared to their respective data range. Sequencing of the neuraminidase of these outliers N2 highlighted several mutations, but none of them were associated with resistance to neuraminidase inhibitors. | [552544] | Drug Info | |
Zanamivir | Influenza virus neuraminidase inhibitors (NAIs) were introduced in clinical practice in various parts of the world since 1999 but were only scarcely distributed in France. Priorto the generalization of zanamivir and oseltamivir utilization in our country, we decided to test a large panel of influenza strains to establish the baseline sensitivity of these viruses to anti-neuraminidase drugs, based upon a fluorometric neuraminidase enzymatic test. Our study was performed on clinical samples collected by practitioners of the GROG network (Groupe R?|gional d'Observation de la Grippe) in the south of France during the 2002-2003 influenza season. Out of 355 isolates tested in the fluorometric neuraminidase activity assay, 267 isolates could be included in inhibition assayagainst anti-neuraminidase drugs. Differences in IC50 range were found according to the subtype and the anti-neuraminidase drug. Influenza B and A/H1N1 viruses appeared to be more sensitive to zanamivir than to oseltamivir (mean B IC50 values: 4.19 nM versus 13 nM; mean H1N1 IC50 values: 0.92 nM versus 1.34 nM), while A/H1N2 and A/H3N2 viruses were more sensitive to oseltamivir than to zanamivir (mean H3N2 IC50 values: 0.67 nM versus 2.28 nM; mean H1N2 IC50 values: 0.9 nM versus 3.09 nM). Out of 128 N2 carrying isolates, 10 isolates had zanamivir or oseltamivir IC50 values in upper limits compared to their respective data range. Sequencing of the neuraminidase of these outliers N2 highlighted several mutations, but none of them were associated with resistance to neuraminidase inhibitors. | [552544] | Drug Info | ||
References | |||||
Ref 552544 | Sensitivity of influenza viruses to zanamivir and oseltamivir: a study performed on viruses circulating in France prior to the introduction of neuraminidase inhibitors in clinical practice. Antiviral Res. 2005 Oct;68(1):43-8. | ||||
Ref 552600 | Optimization of small molecule drugs binding to highly polar target sites: lessons from the discovery and development of neuraminidase inhibitors. Curr Top Med Chem. 2006;6(5):423-34. | ||||
Ref 552544 | Sensitivity of influenza viruses to zanamivir and oseltamivir: a study performed on viruses circulating in France prior to the introduction of neuraminidase inhibitors in clinical practice. Antiviral Res. 2005 Oct;68(1):43-8. | ||||
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 530582 | J Med Chem. 2010 Jan 28;53(2):778-86.Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai. | ||||
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 530017 | Bioorg Med Chem. 2009 Apr 1;17(7):2744-50. Epub 2009 Feb 26.Characteristic of neuraminidase inhibitory xanthones from Cudrania tricuspidata. | ||||
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 552600 | Optimization of small molecule drugs binding to highly polar target sites: lessons from the discovery and development of neuraminidase inhibitors. Curr Top Med Chem. 2006;6(5):423-34. | ||||
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 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 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 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 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 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 530017 | Bioorg Med Chem. 2009 Apr 1;17(7):2744-50. Epub 2009 Feb 26.Characteristic of neuraminidase inhibitory xanthones from Cudrania tricuspidata. | ||||
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 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 530017 | Bioorg Med Chem. 2009 Apr 1;17(7):2744-50. Epub 2009 Feb 26.Characteristic of neuraminidase inhibitory xanthones from Cudrania tricuspidata. | ||||
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 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 530582 | J Med Chem. 2010 Jan 28;53(2):778-86.Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai. | ||||
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 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 530017 | Bioorg Med Chem. 2009 Apr 1;17(7):2744-50. Epub 2009 Feb 26.Characteristic of neuraminidase inhibitory xanthones from Cudrania tricuspidata. | ||||
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 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 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. |
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