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Updated: Jul 4, 2025

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
Published on: May 2, 2025
Recent advances of Pin1 inhibitors as potential anticancer agents
Yiru Bai1, Ziqiao Yuan2, Shuo Yuan1
1Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou 450018, China.
Abstract:
Pin1 (proline isomerase peptidyl-prolyl isomerase NIMA-interacting-1), as a member of PPIase family, catalyzes cis-trans isomerization of pThr/Ser-Pro amide bonds of its substrate proteins, further regulating cell proliferation, division, apoptosis, and transformation. Pin1 is overexpressed in various cancers and is positively correlated with tumor initiation and progression. Pin1 inhibition can effectively reduce tumor growth and cancer stem cell expansion, block metastatic spread, and restore chemosensitivity, suggesting that targeting Pin1 may be an effective strategy for cancer treatment. Considering the promising therapeutic effects of Pin1 inhibitors on cancers, we herein are intended to comprehensively summarize the reported Pin1 inhibitors, mainly highlighting their structures, biological functions and binding modes, in hope of providing a reference for the future drug discovery.
Insights
Pin1 (proline isomerase peptidyl-prolyl isomerase NIMA-interacting-1) is a key regulator in cancer. Inhibiting Pin1 shows promise for cancer treatment by reducing tumor growth and spread.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Pin1 (proline isomerase peptidyl-prolyl isomerase NIMA-interacting-1) is a PPIase enzyme.
- It regulates critical cellular processes including proliferation, division, and apoptosis.
- Pin1 overexpression is linked to cancer initiation, progression, and metastasis.
Purpose of the Study:
- To comprehensively summarize known Pin1 inhibitors.
- To highlight their structures, biological functions, and binding modes.
- To provide a reference for future Pin1 inhibitor drug discovery in cancer treatment.
Main Methods:
- Literature review of reported Pin1 inhibitors.
- Analysis of inhibitor structures and their corresponding biological activities.
- Examination of documented binding modes of Pin1 inhibitors.
Main Results:
- Overview of diverse Pin1 inhibitor structures.
- Correlation between Pin1 inhibition and reduced tumor growth, metastasis, and enhanced chemosensitivity.
- Detailed analysis of specific inhibitor binding interactions.
Conclusions:
- Pin1 inhibitors demonstrate significant therapeutic potential in various cancers.
- Targeting Pin1 is a promising strategy for cancer therapy.
- This review serves as a valuable resource for developing novel Pin1-targeted cancer drugs.
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