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.

Bioorganic Chemistry
|February 7, 2024
PubMed

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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