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Published on: May 14, 2016

Pin1 as an anticancer drug target

Guoyan G Xu1, Felicia A Etzkorn

  • 1Virginia Tech, Department of Chemistry, Blacksburg, Virginia, USA.

Drug News & Perspectives
|November 6, 2009
PubMed

Insights

Pin1 protein isomerase is overexpressed in human cancers and drives tumor growth. Inhibiting Pin1 may offer a novel therapeutic strategy for cancer treatment by inducing apoptosis and blocking cell cycle progression.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Pin1 (Peptidyl-prolyl cis-trans isomerase) catalyzes cis/trans isomerization of phospho-Ser/Thr-Pro bonds.
  • This isomerization affects the function of key substrates like Cdc25C, c-Jun, and p53, influencing critical cellular events.
  • Pin1 overexpression is observed in various human cancers, correlating with elevated cyclin D1 levels and contributing to cell transformation.

Purpose of the Study:

  • To highlight the role of Pin1 in oncogenesis.
  • To establish Pin1 as a potential anticancer therapeutic target.
  • To review existing Pin1 inhibitors and their therapeutic potential.

Main Methods:

  • Literature review of Pin1's enzymatic activity and biological roles.
  • Analysis of Pin1 expression in human cancer tissues.
  • Survey of identified Pin1 inhibitors, including designed and natural products.

Main Results:

  • Pin1 overexpression promotes tumor growth and is linked to cyclin D1 levels.
  • Inhibition of Pin1 induces tumor cell apoptosis and blocks cell cycle progression.
  • Various classes of Pin1 inhibitors have been identified, including small molecules and natural products.

Conclusions:

  • Pin1 is a critical factor in oncogenesis and a promising anticancer drug target.
  • Pin1 inhibitors represent a novel therapeutic approach for cancer treatment.
  • Pin1's role in cell cycle regulation makes it a valuable target for diagnostic and therapeutic strategies.

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