Inhibition of sialidases from viral, bacterial and mammalian sources by analogues of 2-deoxy-2,3-didehydro-N-acetylneuraminic acid modified at the C-4 position
| Autor: | Wendy P. Stewart, Michael S. Pegg, Mark von Itzstein, Wen-Yang Wu, Cindy T. Holzer, Betty Jin |
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| Rok vydání: | 1993 |
| Předmět: |
viruses
Neuraminidase Substrate analog Biology medicine.disease_cause Sialidase Biochemistry Virus Microbiology chemistry.chemical_compound medicine Animals Molecular Biology chemistry.chemical_classification Binding Sites Sheep Bacteria Molecular Structure Cell Biology Clostridium perfringens N-Acetylneuraminic Acid Sialic acid Influenza B virus Enzyme chemistry Vibrio cholerae Influenza A virus Sialic Acids N-Acetylneuraminic acid |
| Zdroj: | Glycoconjugate journal. 10(1) |
| ISSN: | 0282-0080 |
| Popis: | The inhibition of sialidase activity from influenza viruses A and B, parainfluenza 2 virus, Vibrio cholerae, Arthrobacter ureafaciens, Clostridium perfringens, and sheep liver by a range of 2-deoxy-2,3-didehydro-N-acetylneuraminic acid analogues modified at the C-4 position has been studied. All substitutions tested resulted in a decrease in the degree of inhibition of the bacterial and mammalian sialidases. For sialidases from influenza viruses A and B, on the other hand, most of the substitutions tested either had no significant effect on binding or, in the case of the basic amino and guanidino substituents, resulted in significantly stronger inhibition. The results for parainfluenza 2 virus sialidase were mostly intermediate, in that inhibition was neither significantly increased nor decreased by most of the modifications. We conclude that only the influenza A and B sialidase active sites possess acid groups correctly positioned to participate in charge-charge interactions in the region of C-4 of bound substrate, and that the C-4 binding pockets of the bacterial and mammalian sialidases examined are considerably smaller than is observed for either the influenza virus or parainfluenza virus sialidases. |
| Databáze: | OpenAIRE |
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