Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy.

Abstract

Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) specifically binds and isomerizes the phosphorylated serine/threonine-proline (pSer/Thr-Pro) motif, which leads to changes in protein conformation and function. Pin1 is widely overexpressed in cancers and plays an important role in tumorigenesis. Mounting evidence has revealed that targeting Pin1 is a potential therapeutic approach for various cancers by inhibiting cell proliferation, reducing metastasis, and maintaining genome stability. In this review, we summarize the underlying mechanisms of Pin1-mediated upregulation of oncogenes and downregulation of tumor suppressors in cancer development. Furthermore, we also discuss the multiple roles of Pin1 in cancer hallmarks and examine Pin1 as a desirable pharmaceutical target for cancer therapy. We also summarize the recent progress of Pin1-targeted small-molecule compounds for anticancer activity.

• Authors: Hsiang-Hao Chuang, Yen-Yi Zhen, Yu-Chen Tsai, Cheng-Hao Chuang, Ming-Shyan Huang, Michael Hsiao, Chih-Jen Yang
• Journal: Biomedicines (Biomedicines) Vol. 9 Issue 4 (Mar 31 2021) ISSN: 2227-9059 [Print] Switzerland
• PMID: 33807199 (Publication Type: Journal Article, Review)