상세 정보

underline
Metadata Downloads : dc(xml) or Excel
Cited 0 time in scopus ci

Title 

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

Authors 

Y LeeYoung Bae RyuH S YounJ K ChoYoung-Min KimJi-Young ParkWoo Song LeeK H ParkS H Eom

Publisher 

International Union of Crystallography

Issue Date 

2014

Citation 

Acta Crystallographica. Section D, Biological Crystallography, vol. 70, no. 5, pp. 1357-1365

Keywords 

diplaconegeranylated flavonoidNanIsialidasesialidase inhibitor

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.

Citation 

Acta Crystallographica. Section D, Biological Crystallography, 70(5): 1357-1365

ISSN 

0907-4449

Link 

http://dx.doi.org/10.1107/S1399004714002971

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


Files in This Item: SizeFormat
12306.pdf978KbAdobe PDF
qrcode

FusionCharts.
DSpace Software Coptright(c) 2010 MIT and Hewleft-Packard  /  KRIBB-REPOSITORY ( Email:jakim@kribb.re.kr)