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A correlation of endocrine and anticancer effects of some antagonists of GHRH

Magdolna Kovács1, Andrew V Schally, Florian Hohla

  • 1Department of Anatomy, University of Pécs, Medical School, 7624 Pécs, Hungary. magdolna.kovacs@aok.pte.hu

Peptides
|July 17, 2010
PubMed

Insights

Growth hormone-releasing hormone (GHRH) receptor antagonists show anticancer effects. Potent GHRH antagonists strongly inhibit glioblastoma growth by correlating endocrine potency with antiproliferative efficacy.

Area of Science:

  • Endocrinology
  • Oncology
  • Molecular Biology

Background:

  • Growth hormone-releasing hormone (GHRH) receptor antagonists can inhibit experimental tumor growth.
  • Glioblastoma cell lines express pituitary GHRH receptor (pGHRH-R) and its splice variant SV1.
  • The relationship between endocrine potency and anticancer activity of GHRH antagonists requires further investigation.

Purpose of the Study:

  • To investigate the correlation between the endocrine potency and anticancer activity of GHRH antagonists.
  • To compare the effects of GHRH antagonists JV-1-63 and MZJ-7-138 on glioblastoma growth and GH release.

Main Methods:

  • Western blot analysis to detect pGHRH-R and SV1 expression in glioblastoma cell lines.
  • In vivo and in vitro assays to measure GH secretion inhibition by GHRH antagonists.
  • Xenograft model using DBTRG-05 glioblastomas in athymic nude mice to assess tumor growth inhibition.
  • mRNA expression analysis of pGHRH-R and SV1 following antagonist exposure.

Main Results:

  • DBTRG-05 and U-87MG cells express significantly higher levels of pGHRH-R than SV1.
  • The potent GH release inhibitor JV-1-63 reduced glioblastoma tumor growth by 46% in mice.
  • The weaker GH release inhibitor MZJ-7-138 showed no significant effect on tumor growth.
  • GHRH antagonists upregulated pGHRH-R mRNA and downregulated SV1 mRNA expression, with JV-1-63 having a greater effect.

Conclusions:

  • A positive correlation exists between the endocrine potency and antiproliferative efficacy of GHRH antagonists.
  • GHRH antagonists targeting pGHRH-R may represent a promising therapeutic strategy for glioblastomas.
  • The differential regulation of pGHRH-R and SV1 by GHRH antagonists warrants further study.

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