Octapeptide analogues of somatostatin inhibit the clonal growth and vasoactive intestinal peptide-stimulated cyclic AMP formation in human small cell lung cancer cells.

Abstract

Two endocrinologically active octapeptide analogues (BIM-23014 C and BIM-23034) of somatostatin (SRIF) containing either an N- or C-terminal 3-(2-naphthyl)-D-Ala residue were examined for their ability to inhibit the in vitro receptor binding, clonal growth, and vasoactive intestinal peptide (VIP)-stimulated cyclic AMP formation in human small cell lung cancer cell (SCLC) line NCI-H345. Both SRIF peptides inhibited [125I]SRIF(Tyr11)-14 binding with IC50 values in the low nM range. Colony formation in the in vitro SCLC growth assay was also inhibited in the same concentration range, as was VIP-stimulated cyclic AMP formation. Therefore, octapeptide analogues of SRIF function as SCLC SRIF receptor agonists.

• Authors: J E Taylor, J P Moreau, L Baptiste, T W Moody
• Journal: Peptides (Peptides) 1991 Jul-Aug Vol. 12 Issue 4 Pg. 839-43 ISSN: 0196-9781 [Print] United States
• PMID: 1686316 (Publication Type: Journal Article)

Chemical References

• Oligopeptides
• Peptides, Cyclic
• lanreotide
• BIM 23034
• Vasoactive Intestinal Peptide
• Somatostatin
• Cyclic AMP

Topics

• Amino Acid Sequence
• Carcinoma, Small Cell (metabolism, pathology)
• Cell Division (drug effects)
• Cyclic AMP (biosynthesis)
• Humans
• Lung Neoplasms (metabolism, pathology)
• Molecular Sequence Data
• Oligopeptides (pharmacology)
• Peptides, Cyclic
• Somatostatin (analogs & derivatives, pharmacology)
• Tumor Cells, Cultured (drug effects, metabolism, pathology)
• Vasoactive Intestinal Peptide (metabolism)