Abstract
Human colorectal cancer tissue and matched uninvolved mucosa from 21 patients were examined by radioligand displacement for the presence of binding sites for bombesin-like peptides. Five cancers, but no uninvolved mucosa, expressed high-affinity, low-capacity bombesin binding sites (Kd = 6.53 nM, Bmax = 58.6 fmol mg-1 protein) of the gastrin-releasing peptide (GRP)-preferring subtype (IC50 4.8 nM). Bombesin-like peptides may have a role in the pathogenesis of colorectal cancer, and bombesin receptor antagonists may be of value in the treatment of receptor-positive tumours.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aged
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Binding Sites
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Binding, Competitive
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Bombesin / analogs & derivatives
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Bombesin / metabolism
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Colon / metabolism*
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Colon / ultrastructure*
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Colorectal Neoplasms / chemistry*
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Colorectal Neoplasms / metabolism
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Colorectal Neoplasms / ultrastructure*
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Female
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Gastrin-Releasing Peptide
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Humans
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Intestinal Mucosa / metabolism*
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Intestinal Mucosa / ultrastructure*
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Iodine Radioisotopes
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Kinetics
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Male
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Middle Aged
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Peptides / metabolism*
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Radioligand Assay
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Receptors, Bombesin / metabolism*
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Sensitivity and Specificity
Substances
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Iodine Radioisotopes
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Peptides
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Receptors, Bombesin
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bombesin, Tyr(4)-
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Gastrin-Releasing Peptide
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Bombesin