Frizzled Receptors as Potential Therapeutic Targets in Human Cancers

• Main Authors: Chui-Mian Zeng, Zhe Chen, Li Fu
• Format: Article
• Language: English
• Published: MDPI AG 2018-05-01
• Series: International Journal of Molecular Sciences
• Subjects: frizzled receptors; WNT signaling pathway; cancer therapy; antibody; small molecule inhibitor
• Online Access: http://www.mdpi.com/1422-0067/19/5/1543

Frizzled receptors (FZDs) are a family of seven-span transmembrane receptors with hallmarks of G protein-coupled receptors (GPCRs) that serve as receptors for secreted Wingless-type (WNT) ligands in the WNT signaling pathway. Functionally, FZDs play crucial roles in regulating cell polarity, embryonic development, cell proliferation, formation of neural synapses, and many other processes in developing and adult organisms. In this review, we will introduce the basic structural features and review the biological function and mechanism of FZDs in the progression of human cancers, followed by an analysis of clinical relevance and therapeutic potential of FZDs. We will focus on the development of antibody-based and small molecule inhibitor-based therapeutic strategies by targeting FZDs for human cancers.