Issue 57, 2015
From the journal:

Chemical Communications

N-Alkylated aziridines are easily-prepared, potent, specific and cell-permeable covalent inhibitors of human β-glucocerebrosidase†

B. T. Adams,a   S. Niccoli,b   M. A. Chowdhury,a   A. N. K. Esarik,a   S. J. Lees,b   B. P. Rempelc  and  C. P. Phenix*ab  

* Corresponding authors

a Thunder Bay Regional Research Institute, 290 Munro Street, Thunder Bay, Ontario, Canada
E-mail: phenixc@tbh.net

b Northern Ontario School of Medicine, Thunder Bay Campus, 955 Oliver Road, Thunder Bay Ontario, Canada P7B 5E1

c Department of Science, Augustana Faculty, University of Alberta, 4901-46th Ave. Camrose, Alberta, Canada

Abstract

β-Glucocerebrosidase deficiency leads to Gaucher disease and is a potential marker of Parkinson's disease. We have identified N-octyl conduritol aziridine as a potent and specific covalent inactivator of GBA1 in living cells. This compound is a promising lead towards a positron emission tomography probe intended to image GBA1 activity.

Graphical abstract: N-Alkylated aziridines are easily-prepared, potent, specific and cell-permeable covalent inhibitors of human β-glucocerebrosidase

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Article information

DOI
https://doi.org/10.1039/C5CC03828F
Article type
Communication
Submitted
07 May 2015
Accepted
09 Jun 2015
First published
09 Jun 2015

Chem. Commun., 2015,51, 11390-11393

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N-Alkylated aziridines are easily-prepared, potent, specific and cell-permeable covalent inhibitors of human β-glucocerebrosidase

B. T. Adams, S. Niccoli, M. A. Chowdhury, A. N. K. Esarik, S. J. Lees, B. P. Rempel and C. P. Phenix, Chem. Commun., 2015, 51, 11390 DOI: 10.1039/C5CC03828F

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