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GnRH antagonist treatment of malignant adrenocortical tumors

Milena Doroszko1, Marcin Chrusciel1, Joanna Stelmaszewska2

  • 1Institute of Biomedicine, University of Turku, Turku, Finland.

Endocrine-Related Cancer
|November 8, 2018
PubMed

Insights

Gonadotropin-releasing hormone antagonist (CTX) therapy shows promise for adrenocortical carcinomas. CTX treatment reduced tumor growth and promoted apoptosis in GNRHR-positive cancer cells.

Area of Science:

  • Endocrinology
  • Oncology
  • Molecular Biology

Background:

  • Aberrantly expressed G protein-coupled receptors in tumors are potential therapeutic targets.
  • Adrenocortical carcinomas (ACTs) express gonadotropin-releasing hormone receptor (GNRHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR).

Purpose of the Study:

  • To analyze GNRHR, LHCGR, and follicle-stimulating hormone receptor (FSHR) expression in human ACTs.
  • To assess the therapeutic potential of GnRH antagonist cetrorelix acetate (CTX) on ACTs in vitro and in vivo.

Main Methods:

  • In situ hybridization and qPCR for receptor expression analysis in human ACTs.
  • In vitro studies on cultured ACT cells (mouse Cα1, Y-1; human H295R) treated with CTX.
  • In vivo studies using transgenic mice bearing ACTs treated with CTX, human chorionic gonadotropin (hCG), or both.

Main Results:

  • Human ACTs showed GNRHR (54-73%) and LHCGR (77-100%) expression, but no FSHR.
  • CTX treatment in vitro reduced ACT cell viability and proliferation, increasing apoptosis.
  • In vivo, CTX decreased ACT weights and serum hormone levels, downregulating tumor markers and upregulating healthy adrenal genes.

Conclusions:

  • CTX demonstrates direct anti-tumor effects on GNRHR-positive ACT cells, inducing apoptosis.
  • CTX therapy may improve ACT treatment by normalizing gene expression towards a healthy adrenal profile.
  • Targeting GNRHR with CTX represents a potential therapeutic strategy for adrenocortical carcinomas.
Keywords:
GNRHRGnRH antagonistLHCGRcetrorelixtherapy

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