DEPTOR inhibits cell proliferation and confers sensitivity to dopamine agonist in pituitary adenoma

Cancer Lett. 2019 Sep 10:459:135-144. doi: 10.1016/j.canlet.2019.05.043. Epub 2019 Jun 6.

Abstract

DEP domain-containing mechanistic target of rapamycin (mTOR)-interacting protein (DEPTOR) is an important modulator of mTOR, a highly conserved kinase whose hyperactivation is critically involved in a variety of human tumors. The role of DEPTOR playing in pituitary adenoma (PA) is largely unknown. Here, we reported that DEPTOR was downregulated in PA tissues, especially dopamine-resistant prolactinomas. Consistently, overexpression of DEPTOR inhibited pituitary tumor GH3 and MMQ cells proliferation in vitro and in vivo, and sensitized GH3 and MMQ cells to cabergoline (CAB), a dopamine agonist (DA). Conversely, knockdown of DEPTOR promoted GH3 and MMQ cells proliferation, and conferred cells resistance to CAB. Mechanistically, DEPTOR inhibited both mTOR Complex 1 (mTORC1) and 2 (mTORC2) activities in PA cells. In addition, DEPTOR expression level was increased to suppress mTOR kinase activity via decreasing E3 ubiquitin ligase, βTrCP1, in response to CAB. Furthermore, DEPTOR enhanced autophagy-dependent cell death to confer cells sensitivity to CAB. Taken together, our results suggest that DEPTOR may be a potential target for the treatment of PAs.

Keywords: Autophagy; Cabergoline; Prolactinoma; mTOR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenoma / drug therapy*
  • Adenoma / metabolism*
  • Adenoma / pathology
  • Adult
  • Animals
  • Autophagy / drug effects
  • Autophagy / physiology
  • Cell Proliferation / drug effects
  • Cell Proliferation / physiology
  • Dopamine Agonists / pharmacology*
  • Down-Regulation
  • Drug Resistance, Neoplasm
  • Female
  • Heterografts
  • Humans
  • Intracellular Signaling Peptides and Proteins / metabolism*
  • Male
  • Mechanistic Target of Rapamycin Complex 1 / antagonists & inhibitors
  • Mechanistic Target of Rapamycin Complex 1 / metabolism
  • Mechanistic Target of Rapamycin Complex 2 / antagonists & inhibitors
  • Mechanistic Target of Rapamycin Complex 2 / metabolism
  • Mice
  • Mice, Nude
  • Middle Aged
  • Pituitary Gland / metabolism
  • Pituitary Neoplasms / drug therapy*
  • Pituitary Neoplasms / metabolism*
  • Pituitary Neoplasms / pathology
  • Prolactinoma / drug therapy
  • Prolactinoma / metabolism
  • Prolactinoma / pathology
  • Rats

Substances

  • DEPTOR protein, rat
  • Dopamine Agonists
  • Intracellular Signaling Peptides and Proteins
  • DEPTOR protein, human
  • Mechanistic Target of Rapamycin Complex 1
  • Mechanistic Target of Rapamycin Complex 2