STAT3/LKB1 controls metastatic prostate cancer by regulating mTORC1/CREB pathway

Mol Cancer. 2023 Aug 12;22(1):133. doi: 10.1186/s12943-023-01825-8.

Abstract

Prostate cancer (PCa) is a common and fatal type of cancer in men. Metastatic PCa (mPCa) is a major factor contributing to its lethality, although the mechanisms remain poorly understood. PTEN is one of the most frequently deleted genes in mPCa. Here we show a frequent genomic co-deletion of PTEN and STAT3 in liquid biopsies of patients with mPCa. Loss of Stat3 in a Pten-null mouse prostate model leads to a reduction of LKB1/pAMPK with simultaneous activation of mTOR/CREB, resulting in metastatic disease. However, constitutive activation of Stat3 led to high LKB1/pAMPK levels and suppressed mTORC1/CREB pathway, preventing mPCa development. Metformin, one of the most widely prescribed therapeutics against type 2 diabetes, inhibits mTORC1 in liver and requires LKB1 to mediate glucose homeostasis. We find that metformin treatment of STAT3/AR-expressing PCa xenografts resulted in significantly reduced tumor growth accompanied by diminished mTORC1/CREB, AR and PSA levels. PCa xenografts with deletion of STAT3/AR nearly completely abrogated mTORC1/CREB inhibition mediated by metformin. Moreover, metformin treatment of PCa patients with high Gleason grade and type 2 diabetes resulted in undetectable mTORC1 levels and upregulated STAT3 expression. Furthermore, PCa patients with high CREB expression have worse clinical outcomes and a significantly increased risk of PCa relapse and metastatic recurrence. In summary, we have shown that STAT3 controls mPCa via LKB1/pAMPK/mTORC1/CREB signaling, which we have identified as a promising novel downstream target for the treatment of lethal mPCa.

Keywords: AMPK; AR; CREB; LKB1; Metformin; Prostate Cancer; STAT3; mTORC1.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, Non-U.S. Gov't
  • Research Support, N.I.H., Extramural

MeSH terms

  • AMP-Activated Protein Kinases / metabolism
  • Animals
  • Diabetes Mellitus, Type 2*
  • Humans
  • Male
  • Mechanistic Target of Rapamycin Complex 1 / metabolism
  • Metformin* / pharmacology
  • Mice
  • Neoplasm Recurrence, Local
  • Prostatic Neoplasms* / genetics
  • Prostatic Neoplasms* / pathology
  • STAT3 Transcription Factor / genetics
  • STAT3 Transcription Factor / metabolism

Substances

  • AMP-Activated Protein Kinases
  • Mechanistic Target of Rapamycin Complex 1
  • Metformin
  • STAT3 protein, human
  • STAT3 Transcription Factor
  • Stk11 protein, mouse
  • Stat3 protein, mouse