Modulating the wnt signaling pathway with small molecules

作者：Tran Freddi Huan; Zheng Jie J

来源：Protein Science, 2017, 26(4): 650-661.

DOI：10.1002/pro.3122

• Wnt signaling pathway
• small-molecule inhibitors
• cancer
• stem cells
• Frizzled
• Disheveled
• GSK-3 beta
• Axin
• beta-catenin
• T-cell factor/lymphoid enhancer-binding factor
• Porcupine
• and Tankyrase

Wnt signaling is a critical component during embryonic development and also plays an important role in regulating adult tissue homeostasis. Abnormal activation of Wnt signaling has been implicated in many cancers, while reduced activity of Wnt signaling leads to poor wound healing and structural formations. Thus, extensive efforts have been focused on developing small molecules that have potential to either inhibit or activate the pathway, hoping these molecules can offer leads for novel approaches in treating different human diseases. Many small-molecule inhibitors specifically target various elements, such as Frizzled, Disheveled, Porcupine, or Tankyrase, within the Wnt signaling pathways. These small molecules not only have the potential to be further developed as therapeutic reagents, but they may also be used as chemical probes to dissect the underlying mechanism of the Wnt signaling pathways. Therefore, their respective mechanisms and effective dosages are highly pertinent. Aiming to provide an overview of those molecules in a concise, easy-to-use manner, we summarize and organize the current research on them so that it may be helpful for utilization in different studies.

• 出版日期2017-4