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)

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