High-affinity binding sites for gastrin-releasing peptide on human colorectal cancer tissue but not uninvolved mucosa.
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.
Preston
S R
SR
Academic Unit of Surgery, St. James's University Hospital, Leeds, UK.
Woodhouse
L F
LF
Jones-Blackett
S
S
Miller
G V
GV
Primrose
J N
JN
D000368:Aged; D001665:Binding Sites; D001667:Binding, Competitive; D001839:Bombesin / Q000031:analogs & derivatives / Q000378:metabolism; D003106:Colon / Q000378:metabolism* / Q000648:ultrastructure*; D015179:Colorectal Neoplasms / Q000737:chemistry* / Q000378:metabolism / Q000648:ultrastructure*; D005260:Female; D019886:Gastrin-Releasing Peptide; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism* / Q000648:ultrastructure*; D007457:Iodine Radioisotopes; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D010455:Peptides / Q000378:metabolism*; D011869:Radioligand Assay; D018004:Receptors, Bombesin / Q000378:metabolism*; D012680:Sensitivity and Specificity
D007457:Iodine Radioisotopes; D010455:Peptides; D018004:Receptors, Bombesin; C035891:bombesin, Tyr(4)-; D019886:Gastrin-Releasing Peptide; D001839:Bombesin