By R. B. Merrifield (auth.), Ervin G. Erdös, Nathan Back, Federigo Sicuteri, Anne F. Wilde (eds.)
The papers accrued during this quantity have been awarded on the foreign Symposium on Hypotensive Peptides held in Flor ence, Italy, on October 25-29, 1965. the aim of the assembly used to be to collect scientists of fourteen international locations starting from the chemist to the doctor, who often don't communicate a typical language and for whom it'd be rather tough to stick to the newest advancements in fields allied to, yet nonetheless a few what faraway from their uncomplicated curiosity. Their studies sum marized their contemporary development and present achievements, and gave indication of the fashion that destiny learn on hypotensive peptides may possibly take. a variety of elements of the constitution and serve as of brady kinin, kallidin, kallikrein, gastrin, eledoiSin, physalaemin, sub stance P, and comparable ingredients have been mentioned throughout the 9 periods. the 1st consultation was once dedicated to the chemistry of peptides. This used to be in free order by way of experiences facing the constitution of a few more moderen peptides, with kininogen, and with enzymes that liberate or inactivate peptides. accordingly, studies at the physiological, pharmacological, pathological, and scientific value of kinins, kallikrein, and eledoisin have been provided. One whole consultation was once dedicated to substance P. on the remaining consultation movies proven the impression of the peptides at the movement. The appendix of this quantity comprises the document of the overseas Committee on Nomenclature.
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Extra info for Hypotensive Peptides: Proceedings of the International Symposium October 25–29, 1965, Florence, Italy
Example text
Merrifield, R. : Solid-phase peptide synthesis. III. An improved synthesis of bradykinin. Biochemistry 3, 1385 (1964). PEPTIDES AND ANTIBRADYKININ ACTIVITY 31 Merrifield, R. , and J. M. stewart: Automated peptide synthesis. ) 207, 522 (1965). Nicolaides, E. ) D. A. McCarthy, andD. E. Potter: Bradykinin: Configuration of the arginine moieties and biological activity. Biochemistry 4, 190, 1965. , and R. Hempel: Bradykinin, kallidin, and their synthetic analogues. Experientia (Basel) 20, 529 (1964).
Such modifications usually decreased the biological activity of the peptide without increasing its duration of action and without conferring antagonistic activity. It appears that most of the biologically active peptides are highly structure-specific; that is, they must fulfill a multiplicity of steric and functional requirements in order to "fit" their specific receptors and "bind" to them. Optimal fit and effective binding to the receptor sites are absolute conditions for the effectiveness of either long-acting or antagonistic peptIde analogs.
An abbreviated- program for the automated synthesis. For the reagents marked with an asterisk, the pump, shake, and filter operations are repeated in sequence two more times. )- BOC-Phe, CH 2Cl 2 Dicyclohexylcarbodiimide ET3N, DMF HCl, CH 3COOH N02 l l l I Pd-BaSO, Fig. 7. The solid phase synthesis of angiotensinyl-bradykinin. H-Asp-Arg-Val-Tyr-lle-His-Pro-Phe-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH 2, 1H N02 Bz N02 N02 H-Asp-Arg-Val-Tyr-lle-His-Pro-Phe-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH HBr, F 3CCOOH Bz N02 Bz Bz N02 Bz N02 BOC-Asp-Arg-Val-Tyr-lle-His-Pro-Phe-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-Resin J Repeat steps 1, 2, 3 15 more times.