Introduction: Bombesin is a 14-aminoacid peptide isolated from frog skin. The mammalian counterparts of the frog peptide are neuromedin B (NMB) and gastrin-releasing peptide (GRP). Bombesin (BBN) is a peptide showing high affinity for the gastrin releasing peptide receptor (GRPr). Prostate, small cell lung cancer, breast, gastric, and colon cancers are known to over...

Cellular responses elicited by cell surface receptors differ according to stimulus strength. We investigated how the high-affinity receptor for immunoglobulin E (IgE) modulates the response of mast cells to a high- or low-affinity stimulus. Both high- and low-affinity stimuli elicited similar receptor phosphorylation; however, differences were observed in receptor cluster size, mobility, distri...

Cholecystokinin (CCK) is a growth factor for normal pancreas. Nu merous studies also suggest that CCK promotes pancreatic carcinogenesis in the rat. Our previous studies suggested that growth of preneoplastic pancreatic foci was stimulated by CCK more than that of normal pan creas. We hypothesized that such differential growth might be due to increased numbers of CCK receptors in neoplastic tis...

The threshold sensitivity of cardiovascular tissues to a-adrenergic stimulation is determined largely by the affinity of a-adrenergic receptors for agonists. To determine whether changes in a-adrenergic receptor affinity could contribute to the regulation of cardiac and vascular responsiveness, we used the a-adrenergic-selective radioligands, [H]prazosin, [H]-WB-4101, and [H]rauwalscine, to stu...

Cholecystokinin (CCK) is a growth factor for normal pancreas. Nu merous studies also suggest that CCK promotes pancreatic carcinogenesis in the rat. Our previous studies suggested that growth of preneoplastic pancreatic foci was stimulated by CCK more than that of normal pan creas. We hypothesized that such differential growth might be due to increased numbers of CCK receptors in neoplastic tis...

Fluspidine is a high affinity ligand of the σ1 receptor. To further improve affinity, fluspidine analogs were systematically synthesized and screened herein. design modified analogs, docking simulation protein–ligand complex structure was examined. By using developed synthetic strategy involving asymmetric catalytic 1,4-reduction α,β -unsaturated carboxylic esters catalyzed by chiral cobalt com...

Cholecystokinin (CCK) is a growth factor for normal pancreas. Numerous studies also suggest that CCK promotes pancreatic carcinogenesis in the rat. Our previous studies suggested that growth of preneoplastic pancreatic foci was stimulated by CCK more than that of normal pancreas. We hypothesized that such differential growth might be due to increased numbers of CCK receptors in neoplastic tissu...

introduction: neurotensin (nt) is a tridecapeptide that binds specifically to neurotensin receptors. several forms of cancer, including small cell lung cancer, colon, pancreatic and prostate carcinomas especially exocrine pancreatic carcinomas express receptors for neurotensin peptide. radiolabeled neurotensin derivatives with a high affinity for these receptors might be used for scintigraphy. ...

Sphingosylphosphorylcholine (SPC) and lysophosphatidylcholine (LPC) are bioactive lipid molecules involved in numerous biological processes. We have recently identified ovarian cancer G protein-coupled receptor 1 (OGR1) as a specific and high affinity receptor for SPC, and G2A as a receptor with high affinity for LPC, but low affinity for SPC. Among G protein-coupled receptors, GPR4 shares high...