Exploring strategies for targeting oncogenic beta-catenin

一种作用于β-连环蛋白或其下游的抑制剂的发现，不仅将是探索WNT信号在癌症生物学中作用的宝贵工具，而且重要的是将解决依赖于WNT信号的结直肠癌和乳腺癌亚型的更好治疗选择的高度未得到满足的需求。这里概述的项目将进一步加深我们对Beta-catenin中的瞬时或变构口袋是否可以靶向取代BCL9/9L的结合的生物学理解，BCL9/9L是致癌β-catenin活性的重要辅助激活剂。

The discovery of an inhibitor that acts at, or downstream of beta-catenin would not only be a valuable tool for exploring the role of WNT signalling in cancer biology, but importantly would address the high unmet need for better treatment options for colorectal cancer and breast cancer sub-types dependent on WNT-signalling. The project outlined here would further our biological understanding of whether transient or allosteric pockets in Beta-catenin can be targeted to displace binding of BCL9/9L an essential co-activator of oncogenic beta-catenin activity.