Studies on trypsin inhibitors. Part IX. Synthesis and trypsin inhibitory activity of the duopentacontapeptide corresponding to the amino acid sequence of porcine pancreatic secretory trypsin inhibitor II (Kazal)

International Journal of Peptide and Protein Research
R TomatisR Rocchi

Abstract

The synthesis of the protected duopentacontapeptide corresponding to the entire amino acid sequence I-52 of porcine pancreatic secretory trypsin inhibitor II (Kazal type) is described. The benzyloxycarbonyltetradecapeptide tert-butyloxycarbonylhydrazide (sequence 1-14) was selectively deblocked with trifluoroacetic acid and used to acylate, by the azide procedure, the peptide free base corresponding to the sequence 15-52. The isolated material was purified by ion exchange chromatography and the protecting groups were removed by successive treatments with anhydrous hydrogen fluoride, 1 M piperidine and mercuric acetate. F02M phosphate buffer, pH8. Determination of the inhibitory capacity indicated that the synthetic material is about 50% effective, at 30:1 inhibitor:trypsin molar ratio in inhibiting the tryptic hydrolysis of Nalpha-benzoyl-DL-arginine-4-nitroanilide. Full inhibition was achieved at a higher inhibitor:trypsin molar ratio. The stability constants and the standard free energy of binding of the complex between trypsin and the synthetic inhibitor have been determined.

References

Jun 11, 1975·Journal of the American Chemical Society·S Sano, S Kawanishi
Jan 1, 1976·International Journal of Peptide and Protein Research·R RocchiE Menegatti
Sep 24, 1974·Biochemistry·J P VincentM Lazdunski
Jan 1, 1974·International Journal of Peptide and Protein Research·R RocchiR Tomatis
Jul 26, 1972·Journal of the American Chemical Society·D F VeberR Hirschmann
Jan 1, 1964·Biochemical and Biophysical Research Communications·J LenardG P HESS
May 1, 1953·The Biochemical Journal·N M GREEN, E WORK
May 1, 1959·Archives of Biochemistry and Biophysics·G L ELLMAN
Jul 19, 1962·Biochemical and Biophysical Research Communications·K H SHING P HESS
May 14, 1963·Biochimica Et Biophysica Acta·F SANGER, E O THOMPSON
Sep 1, 1948·Journal of the American Chemical Society·L A KAZALR A BRAHINSKY

Related Concepts

Anilides
Metazoa
Hydrogen-Ion Concentration
Hydrolysis
Oxidation-Reduction
Peptide Fragments
Polypeptides
Family suidae
Pancreatic Trypsin Secretory Inhibitor, Kazal
Trypsin Inhibitors

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