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Function of PIN1 in Cancer Development and Its Inhibitors as Cancer Therapeutics

Ji Hoon Yu1, Chun Young Im1, Sang-Hyun Min1

  • 1New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Daegu, South Korea.

Frontiers in Cell and Developmental Biology
|April 8, 2020
PubMed

Insights

Peptidyl-prolyl isomerase (PIN1) targets phosphorylated proteins, impacting cancer development. This review explores PIN1

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Peptidyl-prolyl isomerase (PIN1) regulates protein structure and function by isomerizing phosphorylated serine/threonine-proline motifs.
  • PIN1 dysregulation is implicated in cancer development and progression.
  • PIN1 is frequently overexpressed in various human cancers, promoting tumor growth and cancer stem cell populations.

Purpose of the Study:

  • To review the critical roles of PIN1 in cancer biology.
  • To discuss the potential of PIN1 as a therapeutic target in oncology.
  • To summarize small-molecule compounds targeting PIN1.

Main Methods:

  • Literature review of studies on PIN1 function in cancer.
  • Analysis of the molecular mechanisms by which PIN1 influences oncogenes and tumor suppressors.
  • Compilation of data on existing and emerging PIN1-targeted small-molecule inhibitors.

Main Results:

  • PIN1's specific binding and isomerization of pSer/Thr-Pro motifs alter protein conformation, affecting cellular processes.
  • PIN1 overexpression disrupts the balance between oncogenes and tumor suppressors, driving tumorigenesis.
  • PIN1 contributes to the maintenance and proliferation of cancer stem cells.

Conclusions:

  • PIN1 is a key regulator in cancer development, making it a promising therapeutic target.
  • Targeting PIN1 with small-molecule compounds offers a potential strategy for cancer treatment.
  • Further research into PIN1-targeted therapies is warranted for effective cancer intervention.
Keywords:
PIN1PIN1 inhibitorcancer therapeuticsproline-directed phosphorylationprolyl isomerasetumorigenesis

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