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Nanomolar affinity, iminosugar-based chemical probes for specific labeling of lysosomal glucocerebrosidase.

Abstract：

:Three different photoprobes were synthesized to label beta-glucosidases; one probe was based on glucose, two probes on the iminosugar deoxynojirimycin. The affinity of the probes for three different beta-glucosidases was determined. Furthermore, their labeling efficiencies, binding specificities through competition with deoxynojirimycin, and binding specificities in the presence of cell lysate, were evaluated. Especially one showed very high affinity towards non-lysosomal glucoceramidase (IC(50)=20 nM).

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

van Scherpenzeel M,van den Berg RJ,Donker-Koopman WE,Liskamp RM,Aerts JM,Overkleeft HS,Pieters RJ

doi

10.1016/j.bmc.2009.10.060

subject

Has Abstract

pub_date

2010-01-01 00:00:00

pages

267-73

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00995-X

journal_volume

18

pub_type

杂志文章

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