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Somatostatin analogs and chimeric somatostatin-dopamine molecules differentially regulate human growth hormone and prolactin gene expression and secretion in vitro.

Abstract
We tested effects of selective somatostatin receptor 2 (SST2) agonist BIM-23120, SST5 agonist BIM-23206 and chimeric somatostatin-dopamine molecules (SRIF/DA) BIM-23A760 and BIM-23A761 on GH and PRL secretion and gene expression in human GH/PRL-secreting pituitary tumors in vitro. In "responders" group BIM-23120 suppressed GH levels by 26±4%, BIM-23206 by 31±5%, BIM-23A760 by 23±4%, BIM-23A761 by 39±8% and D(2)-dopamine agonist BIM-53097 by 31±5%. Using real-time PCR we demonstrated that GH inhibition was not accompanied by decreased GH mRNA levels. PRL secretion was inhibited by BIM-23A760 (29±5%), BIM-23A761 (34±4%), BIM-23206 (26±4%) and BIM-53097 (36±2%). SRIF/DA and BIM-53097 also suppressed PRL mRNA levels. Concluding, SST2 and SST5 agonists and SRIF/DA inhibit GH secretion, but do not suppress GH gene transcription. SRIF/DA and BIM-53097 inhibit both PRL secretion and PRL gene expression. SST5 agonist inhibits PRL secretion, but does not suppress PRL gene expression. D(2) affinity is crucial in SRIF/DA action on PRL gene expression.
AuthorsAnna Gruszka, Michael D Culler, Shlomo Melmed
JournalMolecular and cellular endocrinology (Mol Cell Endocrinol) Vol. 362 Issue 1-2 Pg. 104-9 (Oct 15 2012) ISSN: 1872-8057 [Electronic] Ireland
PMID22705877 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2012 Elsevier Ireland Ltd. All rights reserved.
Chemical References
  • BIM 23120
  • BIM 23206
  • BIM-23A761
  • Receptors, Somatostatin
  • Human Growth Hormone
  • Somatostatin
  • Prolactin
  • TBR-760
  • Dopamine
Topics
  • Adenoma (drug therapy, metabolism, pathology)
  • Adult
  • Aged
  • Dopamine (analogs & derivatives, pharmacology)
  • Female
  • Gene Expression Regulation, Neoplastic (drug effects)
  • Human Growth Hormone (genetics, metabolism)
  • Humans
  • Male
  • Middle Aged
  • Pituitary Neoplasms (drug therapy, metabolism, pathology)
  • Prolactin (genetics, metabolism)
  • Receptors, Somatostatin (agonists)
  • Somatostatin (analogs & derivatives, pharmacology)
  • Transcription, Genetic (drug effects)
  • Tumor Cells, Cultured (drug effects)

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