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

Autor: Adams, B. T., Niccoli, S., Chowdhury, M. A., Esarik, A. N. K., Lees, S. J., Rempel, B. P., Phenix, C. P.
Předmět:
Zdroj: Chemical Communications; 7/21/2015, Vol. 51 Issue 57, p11390-11393, 4p
Abstrakt: 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. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index