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PMID: 2999772 Published · ppublish English Journal Article

High-affinity receptors for peptides of the bombesin family in Swiss 3T3 cells.

Zachary I, Rozengurt E

Abstract

Gastrin-releasing peptide (GRP) labeled with 125I at tyrosine-15 (125I-GRP) binds to intact quiescent Swiss 3T3 cells in a specific and saturable manner. Scatchard analysis indicates the presence of a single class of high-affinity binding sites of Kd = 0.5 X 10(-9) M and a value for the number of sites per cell of about 100,000. 125I-GRP binding was not inhibited by other mitogens for these cells, and cell lines that are mitogenically unresponsive to GRP do not exhibit specific GRP binding. Structure-activity relationships show a close parallel between the ability of a range of GRP-related peptides to both inhibit GRP binding and to stimulate mitogenesis. Further, GRP binding is selectively blocked in a competitive fashion by a novel bombesin antagonist, [D-Arg1, D-Pro2, D-Trp7,9, Leu11] substance P. In addition, this compound selectively inhibits GRP and bombesin-induced mitogenesis. These results demonstrate that the mitogenic response of Swiss 3T3 cells to peptides of the bombesin family is mediated by a class of receptors distinct from those of other mitogens for these cells.

MeSH Terms
Animals Bombesin/antagonists & inhibitors Carcinoma, Small Cell/drug therapy Cells, Cultured DNA/biosynthesis Gastrin-Releasing Peptide Iodine Radioisotopes Lung Neoplasms/drug therapy Mice Peptides/metabolism,pharmacology Platelet-Derived Growth Factor/pharmacology Receptors, Bombesin Receptors, Cell Surface/analysis
Chemicals
Iodine Radioisotopes Peptides Platelet-Derived Growth Factor Receptors, Bombesin Receptors, Cell Surface Gastrin-Releasing Peptide DNA Bombesin
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Zachary I
Rozengurt E
References (45)
45 references, click to expand
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Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
Published
1985-11-00
Pages
7616-20
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC391384
Subset
IM
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