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Sitagliptin affects gastric cancer cells proliferation by suppressing Melanoma-associated antigen-A3 expression

Qi Wang1, Pan Lu2, Tao Wang3

  • 1Department of Geriatrics, The First Affiliated Hospital of China Medical University, Shenyang, Liaoning, China.

Cancer Medicine
|April 1, 2020
PubMed

Insights

Sitagliptin, an oral hypoglycemic, inhibits gastric cancer (GC) cell proliferation by regulating the Hippo pathway. It targets Yes-associated protein (YAP) via AMPK, reducing tumor-associated antigen expression.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Abnormal Yes-associated protein (YAP) activation drives tumor proliferation and poor prognosis.
  • Sitagliptin is an oral hypoglycemic agent with potential anti-tumor properties.
  • The effect of sitagliptin on YAP regulation in gastric cancer (GC) is not well understood.

Purpose of the Study:

  • To investigate sitagliptin's effect on GC cell proliferation.
  • To elucidate the role of the Hippo pathway and YAP in sitagliptin's anti-cancer mechanism.
  • To explore the potential of sitagliptin as a therapeutic agent for GC.

Main Methods:

  • Sitagliptin treatment of GC cells.
  • Assessment of cell proliferation and Hippo pathway activity.
  • Western blot analysis to detect YAP phosphorylation and translocation.
  • Measurement of Melanoma-associated antigen-A3 (MAGE-A3) expression.

Main Results:

  • Sitagliptin inhibited GC cell proliferation.
  • Sitagliptin induced YAP phosphorylation in a LATS-dependent manner, promoting cytoplasmic retention.
  • Adenosine 5'-monophosphate-activated protein kinase (AMPK) activation by sitagliptin was crucial for YAP inhibition.
  • Sitagliptin reduced MAGE-A3 expression, a YAP target.

Conclusions:

  • Sitagliptin inhibits GC cell proliferation through the AMPK/YAP pathway.
  • Sitagliptin's mechanism involves YAP phosphorylation, nuclear exclusion, and subsequent reduction in MAGE-A3 expression.
  • Sitagliptin shows potential as an anti-cancer agent for gastric cancer via this pathway.
Keywords:
MAGE-A3YAPgastric cancersitagliptin

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