人β-葡萄糖脑苷脂酶的光开关抑制剂。
Photoswitchable inhibitors of human β-glucocerebrosidase.
作者信息
Davighi Maria Giulia, Clemente Francesca, Matassini Camilla, Cardona Francesca, Nielsen Mogens Brøndsted, Goti Andrea, Morrone Amelia, Paoli Paolo, Cacciarini Martina
机构信息
Department of Chemistry "U. Schiff", University of Florence, via della Lastruccia 3-13, 50019 Sesto F.no (FI), Italy.
Associated with LENS, via N. Carrara 1, 50019 Sesto F.no (FI), Italy.
出版信息
Org Biomol Chem. 2022 Feb 23;20(8):1637-1641. doi: 10.1039/d1ob02159a.
Light-switchable inhibitors of the enzyme β-glucocerebrosidase (GCase) have been developed by anchoring a specific azasugar to a dihydroazulene or an azobenzene responsive moiety. Their inhibitory effect towards human GCase, before and after irradiation are reported, and the effect on thermal denaturation of recombinant GCase and cytotoxicity were studied on selected candidates.
通过将特定氮杂糖锚定到二氢薁或偶氮苯响应部分，已开发出β-葡萄糖脑苷脂酶（GCase）的光开关抑制剂。报告了它们在辐照前后对人GCase的抑制作用，并对选定的候选物研究了其对重组GCase热变性和细胞毒性的影响。
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