Elsevier

Peptides

Volume 12, Issue 1, January–February 1991, Pages 145-149
Peptides

Article
[Des-Met14]Bombesin analogues function as small cell lung cancer bombesin receptor antagonists

https://doi.org/10.1016/0196-9781(91)90181-NGet rights and content

Abstract

A series of bombesin (BN) analogues lacking the C-terminal methionine at the 14 position were evaluated as BN receptor antagonists. [D-Phe6]BN(6–13)amide inhibited specific 125I-GRP binding to lung cancer cell line NCI-H720 with an IC50 value of 12 nM. In contrast, [D-Phe6]BN(6–13)propylamide, butylamide and methylester were more potent with IC50 values of 3, 5 and 5 nM whereas [D-Phe6,Sta13]BN(6–13)amide was less potent with an IC50 value of 180 nM. [D-Phe6]BN(6–13)propylamide antagonized the ability of BN to elevate cytosolic Ca2+, whereas [D-Phe6]BN(6–13)butylamide was a partial agonist. In a small cell lung cancer (SCLC) growth assay, [D-Phe6]BN(6–13)propylamide inhibited colony formation. In summary, BN analogues which lack a C-terminal methionine may function as useful SCLC BN receptor antagonists.

References (24)

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