The role of Pin1 in the development and treatment of cancer

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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.

Archives of Pharmacal Research
|August 31, 2016
PubMed

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.
Keywords:
Cancer-driving pathwaysPin1Pin1 inhibitorProline-directed phosphorylationProlyl isomeraseTumorigenesis

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