About: Structural basis of sialidase in complex with geranylated flavonoids as potent natural inhibitors

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About: Structural basis of sialidase in complex with geranylated flavonoids as potent natural inhibitors Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Structural basis of sialidase in complex with geranylated flavonoids as potent natural inhibitors
Creator	Park, Ji-Young Lee, Youngjin Youn, Hyung-Seop Eom, Soo Kim, Young Lee, Woo Park, Ki Ryu, Young Cho, Keun Jung, ‡
source	Medline; PMC
abstract	Sialidase catalyzes the removal of a terminal sialic acid from glycoconjugates and plays a pivotal role in nutrition, cellular interactions and pathogenesis mediating various infectious diseases including cholera, influenza and sepsis. An array of antiviral sialidase agents have been developed and are commercially available, such as zanamivir and oseltamivir for treating influenza. However, the development of bacterial sialidase inhibitors has been much less successful. Here, natural polyphenolic geranylated flavonoids which show significant inhibitory effects against Cp-NanI, a sialidase from Clostridium perfringens, are reported. This bacterium causes various gastrointestinal diseases. The crystal structure of the Cp-NanI catalytic domain in complex with the best inhibitor, diplacone, is also presented. This structure explains how diplacone generates a stable enzyme–inhibitor complex. These results provide a structural framework for understanding the interaction between sialidase and natural flavonoids, which are promising scaffolds on which to discover new anti-sialidase agents.
has issue date	2014-04-30(xsd:dateTime)
bibo:doi	10.1107/s1399004714002971
bibo:pmid	24816104
has license	cc-by
sha1sum (hex)	051cf89045450e5eff3fc9ba4fdc518fe1d623b8
schema:url	https://doi.org/10.1107/s1399004714002971
resource representing a document's title	Structural basis of sialidase in complex with geranylated flavonoids as potent natural inhibitors
has PubMed Central identifier	PMC4014123
has PubMed identifier	24816104
schema:publication	Acta Crystallogr D Biol Crystallogr
resource representing a document's body	covid:051cf89045450e5eff3fc9ba4fdc518fe1d623b8#body_text
is schema:about of	named entity 'FLAVONOIDS' named entity 'INHIBITORS' named entity 'COMPLEX' named entity 'STRUCTURAL' named entity 'SIALIDASE' named entity 'BIOLOGICAL' named entity 'NATURAL' named entity 'CRYSTALLOGRAPHY' named entity 'BASIS' named entity 'Biological' named entity 'flavonoids' named entity 'natural' named entity 'inhibitors' named entity 'sialidase' named entity 'PDB' named entity 'W1, W2 and W3' named entity 'pH 9' named entity 'homology' named entity 'diffusion' named entity 'Neu2' named entity 'Neu2' named entity 'conformational change' named entity 'structure-based' named entity 'hydrogen-bond' named entity 'substrate' named entity 'lysosomes' named entity 'sialidases' named entity 'centrifugation' named entity 'biofilm' named entity 'hydrophobic' named entity 'flavonoids' named entity 'sialidases' named entity 'pathogenic bacteria' named entity 'enterotoxaemia' named entity 'gastrointestinal diseases' named entity 'Neu3' named entity '5.0' named entity 'butyrylcholinesterase' named entity 'nonlinear regression' named entity 'lead compound' named entity 'sialidase' named entity 'Neu4' named entity 'binding affinity' named entity 'pathogens' named entity 'Neu5Ac' named entity 'bacteria' named entity 'protein' named entity 'Neu1' named entity 'sialidase' named entity 'competitive inhibition' named entity 'pathogenesis' named entity 'sialidases' named entity 'sialidase' named entity 'w/v' named entity 'influenza' named entity 'N-acetylneuraminic acid' named entity 'influenza' named entity 'sialidase' named entity 'polyethylene glycol' named entity 'Neu5Ac' named entity 'sialic acids' named entity 'Neu1' named entity 'severe acute respiratory syndrome' named entity 'antiviral' named entity 'substrate' named entity 'ammonium sulfate' named entity 'SARS' named entity 'flavonoid' named entity 'gastrointestinal diseases' named entity 'flavonoids' named entity 'CCP4' named entity 'imidazole'

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