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. 2015 Jul 21;51(57):11390-3.
doi: 10.1039/c5cc03828f.

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

B T Adams  1 , S Niccoli, M A Chowdhury, A N K Esarik, S J Lees, B P Rempel, C P Phenix
Affiliations

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

B T Adams et al. Chem Commun (Camb). .

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.

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