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Anti-influenza virus activity of benzo[d]thiazoles that target heat shock protein 90Lamut, Andraž ...Seasonal or pandemic influenza virus infections are a worldwide health problem requiring antiviral therapy. Since virus resistance to the established neuraminidase inhibitors and novel polymerase ... inhibitors is growing, new drug targets are needed. Heat shock protein 90 (Hsp90) is associated with several aspects of the influenza virus life cycle, and is considered a relevant host cell target. We report here on a series of benzo[d]thiazole and 4,5,6,7-tetrahydrobenzo[d]thiazole derivatives with robust and selective activities against influenza A (H1N1, H3N2) and influenza B viruses. Two compounds, 1 and 4, have low micromolar EC50 values and show high binding affinities for Hsp90, which suggests that inhibition of Hsp90 is the mechanism underlying their antiviral effects. These compounds represent suitable scaffolds for designing novel Hsp90 inhibitors with favourable activities against influenza virus.Source: Bioorganic chemistry. - ISSN 0045-2068 (Vol. 98, 2020, str. 1-8)Type of material - article, component part ; adult, seriousPublish date - 2020Language - englishCOBISS.SI-ID - 4892017
Author
Lamut, Andraž |
Gjorgjieva, Marina |
Naesens, Lieve |
Liekens, Sandra |
Lillsunde, Katja-Emilia |
Tammela, Päivi |
Kikelj, Danijel |
Tomašič, Tihomir
Topics
Gripa |
Virusne bolezni |
antiviral agent |
benzo[d]thiazole |
Hsp90 |
influenza virus |
anti-influenčna aktivnost |
pandemična gripa |
[d]benzotiazol
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Author | Lamut, Andraž ... |
Title | Anti-influenza virus activity of benzo[d]thiazoles that target heat shock protein 90 |
Publication date | |
COBISS.SI-ID | 4892017 |
Publication version in repository | Publisher's version |
Publication licence | Unidentified |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
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Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Razvoj novih zaviralcev Hsp90 s protitumornim delovanjem | J1-1717-2019 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Phenotypic biosensor-based HTS and mode of action analysis by metabolomics and transcriptomics for enhancing antimicrobial drug discovery against Gram-negative bacteria | 277001 |
Academy of Finland |
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New antimicrobials against Gram-positive bacteria | 304697 |
Academy of Finland |
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Phenotypic biosensor-based HTS and mode of action analysis by metabolomics and transcriptomics for enhancing antimicrobial drug discovery against Gram-negative bacteria | 312503 |
Academy of Finland |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Lamut, Andraž | 37669 |
Gjorgjieva, Marina | 50173 |
Naesens, Lieve | ![]() |
Liekens, Sandra | ![]() |
Lillsunde, Katja-Emilia | ![]() |
Tammela, Päivi | ![]() |
Kikelj, Danijel | 01463 |
Tomašič, Tihomir | 28334 |
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