Modulation of GSK-3βactivity in cancer treatment
10.3969/j.issn.1001-1978.2014.06.001
- VernacularTitle:GSK-3β活性调节与肿瘤治疗
- Author:
Li TAO
;
Xiaobo SHENG
;
Yuping LIU
;
Zhonghong WEI
;
Aiyun WANG
;
Yin LU
- Publication Type:Journal Article
- Keywords:
glycogen synthase kinase 3β;
Wnt/β-catenin signa-ling pathway;
insulation mechanisms;
drug design;
substrate competitive inhibitor;
cancer treatment
- From:
Chinese Pharmacological Bulletin
2014;(6):741-743,744
- CountryChina
- Language:Chinese
-
Abstract:
As the major member of serine/threonine protein ki-nases family, glycogen synthase kinase 3β ( GSK-3β) has well characterized roles in the development of a variety of diseases. However, it is noticed that modulation of GSK-3β in tumor pro-gress is two-faced. Once the activity of GSK-3βas a“pro-onco-genic factor” is inhibited, opposing role as a“tumor suppressor”can also be disrupted, which will trigger the consequent side effect on activation of Wnt/β-catenin signaling pathway. The is-sue has placed a major obstacle to anti-GSK-3β in cancer treat-ment. In fact, functional compartmentalization of a large number of intracellular signaling events cross-talked with GSK-3β can prevent their mutual interference and determine the cell fate. Therefore, understanding the specific mechanisms of GSK-3β in regulation of diverse signaling systems or refinement of a sub-strate competitive inhibitor may have great significance to exploit approaches selectively target GSK-3β in tumor treatment.
