Antagonists of bombesin/gastrin-releasing peptide inhibit growth of JAR human choriocarcinoma cells and production of cyclic AMP in vitro

T. Ertl, Y. Qin, K. Groot, J. Horváth, R. Cai, A. V. Schally

Research output: Contribution to journalArticle

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Abstract

The effects of bombesin/GRP antagonists RC-3095 and RC-3940-II on the in vitro proliferation of JAR human choriocarcinoma cells were evaluated. Antagonists RC-3095 and RC-3940-II effectively inhibited growth of cultured JAR cells, inducing a dose- and time-dependent decrease in the number of treated cells. RC-3940-II was more potent than RC-3095 in inhibiting the growth of JAR cells. Addition of RC-3940-II to JAR cell cultures significantly inhibited the cell proliferation at concentrations as low as 1 nM, while 10 nM RC-3095 was required for a similar effect. Receptor binding studies demonstrated the presence of a single class of binding sites for bombesin on JAR cells. RC-3940-II displaced [125I]Tyr4-bombesin bound to the receptors. When JAR cells were cultured in the presence of 10 nM RC-3095 or RC-3940-II for 72 h, cAMP levels in the incubation medium were decreased by 70-80%, compared to the controls. These results suggest that bombesin/GRP antagonists RC-3095 and RC-3940-II inhibit the proliferation of JAR human chorionic adenocarcinoma cells in vitro and that these effects may involve intracellular cAMP pathway.

Original languageEnglish
Pages (from-to)547-553
Number of pages7
JournalInternational Journal of Oncology
Volume6
Issue number3
Publication statusPublished - 1995

Fingerprint

Gastrin-Releasing Peptide
Bombesin
Choriocarcinoma
Cyclic AMP
Growth
Cultured Cells
In Vitro Techniques
Hca(6)-Leu(13)-psi(CH2N)-Tac(14)-bombesin(6-14)
Tpi(6)-Leu(13)-psi(CH2NH)-Leu(14)-bombesin (6-14)
Adenocarcinoma
Cell Culture Techniques
Cell Count
Binding Sites
Cell Proliferation

Keywords

  • bombesin
  • bombesin antagonist
  • bombesin receptor
  • cancer cell growth
  • choriocarcinoma
  • cyclic AMP
  • gastrin-releasing peptide

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

Antagonists of bombesin/gastrin-releasing peptide inhibit growth of JAR human choriocarcinoma cells and production of cyclic AMP in vitro. / Ertl, T.; Qin, Y.; Groot, K.; Horváth, J.; Cai, R.; Schally, A. V.

In: International Journal of Oncology, Vol. 6, No. 3, 1995, p. 547-553.

Research output: Contribution to journalArticle

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abstract = "The effects of bombesin/GRP antagonists RC-3095 and RC-3940-II on the in vitro proliferation of JAR human choriocarcinoma cells were evaluated. Antagonists RC-3095 and RC-3940-II effectively inhibited growth of cultured JAR cells, inducing a dose- and time-dependent decrease in the number of treated cells. RC-3940-II was more potent than RC-3095 in inhibiting the growth of JAR cells. Addition of RC-3940-II to JAR cell cultures significantly inhibited the cell proliferation at concentrations as low as 1 nM, while 10 nM RC-3095 was required for a similar effect. Receptor binding studies demonstrated the presence of a single class of binding sites for bombesin on JAR cells. RC-3940-II displaced [125I]Tyr4-bombesin bound to the receptors. When JAR cells were cultured in the presence of 10 nM RC-3095 or RC-3940-II for 72 h, cAMP levels in the incubation medium were decreased by 70-80{\%}, compared to the controls. These results suggest that bombesin/GRP antagonists RC-3095 and RC-3940-II inhibit the proliferation of JAR human chorionic adenocarcinoma cells in vitro and that these effects may involve intracellular cAMP pathway.",
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AU - Groot, K.

AU - Horváth, J.

AU - Cai, R.

AU - Schally, A. V.

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