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

Monique van Scherpenzeel; Richard J. B. H. N. van den Berg; Wilma E. Donker-Koopman; Rob M. J. Liskamp; Johannes M. F. G. Aerts; Herman S. Overkleeft; Roland J. Pieters

doi:10.1016/j.bmc.2009.10.060

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

Monique van Scherpenzeel
, Richard J. B. H. N. van den Berg
, Wilma E. Donker-Koopman
, Rob M. J. Liskamp
, Johannes M. F. G. Aerts
, Herman S. Overkleeft
, Roland J. Pieters

Research output: Contribution to journal › Article › Academic › peer-review

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)=20nM)

Original language	English
Pages (from-to)	267-273
Journal	Bioorganic & medicinal chemistry
Volume	18
Issue number	1
DOIs	https://doi.org/10.1016/j.bmc.2009.10.060
Publication status	Published - 2010

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10.1016/j.bmc.2009.10.060

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@article{6d5d8c92bebf478885185f230384b66e,

title = "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)=20nM)",

author = "\{van Scherpenzeel\}, Monique and \{van den Berg\}, \{Richard J. B. H. N.\} and Donker-Koopman, \{Wilma E.\} and Liskamp, \{Rob M. J.\} and Aerts, \{Johannes M. F. G.\} and Overkleeft, \{Herman S.\} and Pieters, \{Roland J.\}",

year = "2010",

doi = "10.1016/j.bmc.2009.10.060",

language = "English",

volume = "18",

pages = "267--273",

journal = "Bioorganic \& medicinal chemistry",

issn = "0968-0896",

publisher = "Elsevier Limited",

number = "1",

}

TY - JOUR

T1 - Nanomolar affinity, iminosugar-based chemical probes for specific labeling of lysosomal glucocerebrosidase

AU - van Scherpenzeel, Monique

AU - van den Berg, Richard J. B. H. N.

AU - Donker-Koopman, Wilma E.

AU - Liskamp, Rob M. J.

AU - Aerts, Johannes M. F. G.

AU - Overkleeft, Herman S.

AU - Pieters, Roland J.

PY - 2010

Y1 - 2010

N2 - 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)=20nM)

AB - 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)=20nM)

U2 - 10.1016/j.bmc.2009.10.060

DO - 10.1016/j.bmc.2009.10.060

M3 - Article

C2 - 19931460

SN - 0968-0896

VL - 18

SP - 267

EP - 273

JO - Bioorganic & medicinal chemistry

JF - Bioorganic & medicinal chemistry

IS - 1

ER -

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

Abstract

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