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Molecular BioSystems Vol - 7 Issue - 3

Molecular BioSystems Vol - 7 Issue - 2

Molecular BioSystems Vol -6

Molecular BioSystems Vol -5

Molecular BioSystems Vol -4

Molecular BioSystems Vol -3

Molecular BioSystems Vol -2

Identifying selective inhibitors against the human cytosolic sialidase NEU2 by substrate specificity studies

Content Provider	Royal Society of Chemistry (RSC)
Author	Chen, Yi Chen, Xi Cao, Hongzhi Li, Yanhong Qu, Jingyao Lau, Kam Sugiarto, Go Thon, Vireak Yu, Hai
Copyright Year	2011
Abstract	Aberrant expression of human sialidases has been shown to associate with various pathological conditions. Despite the effort in the sialidase inhibitor design, less attention has been paid to designing specific inhibitors against human sialidases and characterizing the substrate specificity of different sialidases regarding diverse terminal sialic acid forms and sialyl linkages. This is mainly due to the lack of sialoside probes and efficient screening methods, as well as limited access to human sialidases. A low cellular expression level of the human sialidase NEU2 hampers its functional and inhibitory studies. Here we report the successful cloning and expression of the human sialidase NEU2 in E. coli. About 11 mg of soluble active NEU2 was routinely obtained from 1 L of E. coli cell culture. Substrate specificity studies of the recombinant human NEU2 using twenty p-nitrophenol (pNP)-tagged α2–3- or α2–6-linked sialyl galactosides containing different terminal sialic acid forms including common N-acetylneuraminic acid (Neu5Ac), non-human N-glycolylneuraminic acid (Neu5Gc), 2-keto-3-deoxy-D-glycero-D-galacto-nonulosonic acid (Kdn), or their C5-derivatives in a microtiter plate-based high-throughput colorimetric assay identified a unique structural feature specifically recognized by the human NEU2 but not two bacterial sialidases. The results obtained from substrate specificity studies were used to guide the design of a sialidase inhibitor that was selective against human NEU2. The selectivity of the inhibitor was revealed by the comparison of sialidase crystal structures and inhibitor docking studies.
Starting Page	1060
Ending Page	1072
Page Count	13
File Format	HTM / HTML PDF
ISSN	1742206X
Volume Number	7
Issue Number	4
Journal	Molecular BioSystems
DOI	10.1039/c0mb00244e
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Open
Subject Keyword	Cell culture 4-Nitrophenol Escherichia coli L of Enzyme inhibitor Sialidase
Content Type	Text
Resource Type	Article
Subject	Molecular Biology Biotechnology

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Identifying selective inhibitors against human cytosolic sialidase NEU2 by substrate specificity studiesξ

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