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

van Scherpenzeel, M., van den Berg, R.J.B.H.N., Donker-Koopman, W.E., Liskamp, R.M.J. , Aerts, J.M.F.G., Overkleeft, H.S. and Pieters, R.J. (2010) Nanomolar affinity, iminosugar-based chemical probes for specific labeling of lysosomal glucocerebrosidase. Bioorganic and Medicinal Chemistry, 18(1), pp. 267-273. (doi:10.1016/j.bmc.2009.10.060)

Full text not currently available from Enlighten.

Abstract

Three different photoprobes were synthesized to label β-glucosidases; one probe was based on glucose, two probes on the iminosugar deoxynojirimycin. The affinity of the probes for three different β-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 (IC50 = 20 nM).

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Liskamp, Professor Robert
Authors: van Scherpenzeel, M., van den Berg, R.J.B.H.N., Donker-Koopman, W.E., Liskamp, R.M.J., Aerts, J.M.F.G., Overkleeft, H.S., and Pieters, R.J.
College/School:College of Science and Engineering > School of Chemistry
Journal Name:Bioorganic and Medicinal Chemistry
ISSN:0968-0896
ISSN (Online):1464-3391

University Staff: Request a correction | Enlighten Editors: Update this record