| [Des-Met14]bombesin analogues function as small cell lung cancer bombesin receptor antagonists. | |
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MedLine Citation:
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PMID: 1646997 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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J Staley; D Coy; J E Taylor; S Kim; T W Moody |
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Publication Detail:
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Type: Journal Article; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: Peptides Volume: 12 ISSN: 0196-9781 ISO Abbreviation: Peptides Publication Date: 1991 Jan-Feb |
Date Detail:
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Created Date: 1991-07-22 Completed Date: 1991-07-22 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 8008690 Medline TA: Peptides Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 145-9 Citation Subset: IM |
Affiliation:
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Department of Biochemistry & Molecular Biology, George Washinton University School of Medicine and Health Sciences, Washington, DC 20037. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Bombesin
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analogs & derivatives*,
metabolism,
pharmacology Carcinoma, Small Cell / metabolism*, pathology Cell Division / drug effects Humans Lung Neoplasms / metabolism*, pathology Receptors, Bombesin Receptors, Neurotransmitter / antagonists & inhibitors* Second Messenger Systems / drug effects Tumor Cells, Cultured |
| Grant Support | |
ID/Acronym/Agency:
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CA-45153/CA/NCI NIH HHS; CA-53477/CA/NCI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Receptors, Bombesin; 0/Receptors, Neurotransmitter; 31362-50-2/Bombesin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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