Structure-function relationships in gastrin-like peptides

摘要: As the work leading to elucidation of structures hog gastrins was nearing completion and synthesis hormones being planned, it became clear that glycine residue at position 13 offered a convenient dividing point in synthesis. Our colleagues Liverpool subsequently concerned with 1-13 fragments we 14-17 fragment, Try-Met-Asp-Phe-NH 2 , molecules. Not long afterwards tetrapeptide amide had been synthesised found by Tracy & Gregory (1964) possess all physiological properties natural hormones. The finding activity so small ‘stump’ molecule scope for an investigation structure-function relationships on scale not hitherto possible polypeptide We attached value such two accounts. First, results might contribute towards our knowledge mode action general. Secondly, conclusions enabling more rational approach design inhibitors be provided. Both expectations were clearly pertinent objective researches—the development therapeutic agents assessment control gastric secretory function humans. For purposes prepared about 500 derivatives or analogues comprising: ( ) various N -terminally acylated amide, ranging from simple like acetyl (Ac-Try-Met-Asp-Phe-NH2) extended peptides hexadecapeptide sequence (2-17) human gastrin (H-Gly-Pro-Try-Leu-(Glu)5-Ala-Tyr-Gly-Try-Met-Asp-Phe-NH2), b )analogues derived single replacements five main positions (the four amino-acid terminal positions), c positions. tripeptide H-Met-Asp-Phe-NH2, dipeptide H-Asp-Phe-NH2, these compounds also examined, but since general devoid biological they will discussed. Thirty-three selected examined conscious dog Physiological Laboratory, University Liverpool; describing their influence acid secretion, motility, intestinal pancreatic pepsin secretion have reported (Morley, 1965). present paper concerns obtained rats own laboratories larger group respect acid-stimulatory only.