The role of Pin1 in the development and treatment of cancer
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Updated: Mar 15, 2026

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog
Published on: November 5, 2014
Sang-Hyun Min1, Xiao Zhen Zhou2, Kun Ping Lu2,3
1New Drug Development Center, DGMIF, 80 Cheombok-ro Dong-gu, Daegu, 701-310, Korea. shmin03@dgmif.re.kr.
Abstract:
Protein phosphorylation and post-phosphorylation events regulate many cellular signaling pathways. Peptidyl-prolyl isomerase (Pin1) is the only peptidyl-prolyl cis/trans isomerase that interacts with numerous oncogenic or tumor suppressive phosphorylated proteins, causes conformational changes in target proteins, and eventually regulates the activities of such proteins. These alterations in activity play a pivotal role in tumorigenesis. Since Pin1 is overexpressed and/or activated in various types of cancers, and the dysregulation of proline-directed phosphorylation contributes to tumorigenesis, Pin1 represents an attractive target for cancer therapy. This review will describe the role of Pin1 in cancer and the current status of Pin1 inhibitor development.
Insights
Peptidyl-prolyl isomerase (Pin1) regulates proteins involved in cancer. Inhibiting Pin1, which is overexpressed in many cancers, shows promise for new cancer therapies.
Area of Science:
- Molecular Biology
- Biochemistry
- Cancer Biology
Background:
- Protein phosphorylation and post-translational modifications are key regulators of cellular signaling pathways.
- Peptidyl-prolyl isomerase (Pin1) is a unique enzyme that isomerizes proline-containing phosphorylated motifs.
- Pin1 interacts with numerous phosphorylated proteins, influencing their conformation and activity, which is critical in tumorigenesis.
Purpose of the Study:
- To review the critical role of Pin1 in various types of cancer.
- To discuss the current development status of Pin1 inhibitors as a potential cancer therapeutic strategy.
Main Methods:
- Literature review of studies on Pin1 function in cancer.
- Analysis of the role of proline-directed phosphorylation in tumorigenesis.
- Overview of current Pin1 inhibitor development.
Main Results:
- Pin1 is overexpressed and/or activated in a wide range of cancers.
- Dysregulation of proline-directed phosphorylation by Pin1 contributes significantly to cancer development.
- Pin1's role in regulating oncogenic and tumor-suppressive proteins makes it a viable therapeutic target.
Conclusions:
- Pin1 is a crucial mediator in cancer development due to its regulation of key signaling proteins.
- Targeting Pin1 with inhibitors represents a promising therapeutic avenue for various cancers.
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