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基于α-甘露糖苷酶抑制作用的新型抗癌策略研究。

Studies toward new anti-cancer strategies based on alpha-mannosidase inhibition.

作者信息

Gerber-Lemaire Sandrine, Juillerat-Jeanneret Lucienne

机构信息

Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne, Batochime, CH-1015 Lausanne, Switzerland.

出版信息

Chimia (Aarau). 2010;64(9):634-9. doi: 10.2533/chimia.2010.634.

Abstract

Changes in the glycosylation pattern of cellular glycoproteins constitute a hallmark in human cancer and influence tumor progression, suggesting that inhibitors of selected glycosidases may control cancer progression. Following the studies on swainsonine, a natural inhibitor of Golgi alpha-mannosidase II, which highlighted the inhibition of cellular mannosidases as a potential innovative approach for the treatment of cancer, several dihydroxylated pyrrolidines and analogues were developed as new potent inhibitors of alpha-mannosidases II able to induce antiproliferative effects in human cancer cells.

摘要

细胞糖蛋白糖基化模式的改变是人类癌症的一个标志,并影响肿瘤进展,这表明特定糖苷酶的抑制剂可能控制癌症进展。在对戈谢氏病天然抑制剂苦马豆素的研究之后,该研究强调抑制细胞甘露糖苷酶是一种潜在的创新癌症治疗方法,几种二羟基化吡咯烷及其类似物被开发为新型高效的α-甘露糖苷酶II抑制剂,能够在人类癌细胞中诱导抗增殖作用。

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