Peptide enzyme inhibitors

Abstract

Abstract WHEREIN Y IS LYS OR GLU, 11. AN UNDECAPEPTIDE OF THE FORMULA PGLU-TRP-PRO-ARG-PRO-V-PRO-W-ILE-PRO-PRO WHEREIN V IS THR OR GLY AND W IS GLN OR GLU, 12 A. TRIDECAPEPTIDE OF THE FORMULA PGLU-TRP-PRO-NLE-T-PRO-PRO WHEREIN T IS AS DEFINED ABOVE, PGLU-TRP-PRO-ARG-PRO-GLU-PHE-PRO-PRO, PGLU-TRP-PRO-ARG-PRO-LYS-PHE-ALA-PRO, PGLU-TRP-PRO-D-ARG-PRO-GLN-ILLE-PRO-PRO, PGLU-TRP-PRO-AGR-PRO-GLN-PHE-PRO-PRO, PGLU-TRP-PRO-GLY-PRO-GLU-ILE-PRO-PRO, PGLU-LYS-PHE-ALA-PRO-GLN-ILE-PRO-PRO, 10. A DECAPEPTIDE OF THE FORMULA PGLU-K-TRP-PRO-ARG-PRO-GLN-ILE-PRO-PRO WHEREIN K, P AND Q ARE AS DEFINED ABOVE, PGLU-U-TRP-PRO-ARG-PRO-GLN-ILE-PRO-PRO THE ENZYMATIC CONVERSION OF ANGIOSTENSIN I INTO ANTIOTENSIN II IS INHIBITED BY A PEPTIDE OR AN ACYLATED PEPTIDE HAVING ONE OF THE FOLLOWING AMINO ACID SEQUENCES: 1. AN ACYLATED TRIPEPTIDE OF THE FORMULA CHC-PHE-ALA-PRO WHEREIN CAC IS CHLOROACETIC ACID, 2. A TETRAPEPTIDE OF THE FORMULA PGLU-TRP-ALA-PRO OR PGLU-LYS-TRP-PRO, 3. AN ACYLATED TETRAPEPTIDE OF THE FORMULA DAC-FLY-ALA-PRO OR A-LYS-PHE-ALA-PRO WHEREIN DAC IS DIAZOACETIC ACID, AND A IS CHLOROACETIC ACID, CYCLOBUTYLCARBOXYLIC ACID, CYCLOPENTYLCARBOXYLIC ACID OR CYCLOHEXYLCARBOXYLIC ACID, 4. A PENTAPEPTIDE OF THE FORMULA PGLU-C-TRP-ALA-PRO WHEREIN B IS LYS, NLE, GLU OR GIN, PGLU-C-TRP-ALA-PRO WHEREIN C IS NLE, HIS, ORN OR ARG, N''PGLU-LYS-TRP-ALA-PRO,PGLU-LYS-E-ALA-PRO WHEREIN E IS HIS , ILE, PRO, SER OR 3-AMINO-4-PHENYL-BUTYRIC ACID, PGLU-LYS-PHE-F-PRO WHEREIN G IS ALA, ASP OR GLU, PGLU-LYS-PHE-ALA-G WHEREIN W IS AS DEFINED ABOVE. WHEREIN G IS ALA, ASP OR GLU, PGLU-LYS-TRP-H WHEREIN H IS ILE-PRO, THR-PRO-ALA-GLY OR ALA-SAR, PGLU-TRP-PRO-J-PRO WHEREIN J IS HIS, LYS OR GLY, 5. AN ACYLATED PENTAPEPTIDE OF THE FORMULA DAC-GLY-GLY-PHE-ALA-PRO WHEREIN DAC IS DIAZOACETIC ACID, 6. A HEXAPEPTIDE OF THE FORMULA PGLU-LYS-PHE-ALA-PRO-PRO, PGLU-K-TRP-PRO-ARG-PRO WHEREIN K IS ASN, NLE OR SER, PGLU-NLE-TRP-PRO-L-PRO WHEREIN L IS HIS OR GLY, PGLU-ASN-TRP-PRO-M-PRO WHEREIN M IS LYS OR GLY, 7. AN OCTAPEPTIDE OF THE FORMULA PGLU-ILE-PRO-PRO-LYS-PHE-ALA-PRO, 8. AN ACYLATED OCTAPEPTIDE OF THE FORMULA N-O-PRO-ARG-PRO-GLN-ILE-PRO-PRO WHEREIN N IS CYCLOBUTYLCARBOXYLIC ACID, CYCLOPENTYLCARBOXYLIC ACID OR CYCLOHEXYLCARBOXYLIC ACID AND O IS TRP, TYR, -TYR(-BZL)- PHE, GLY, LEU, OR D-TRP, N-TRP-PRO-GLY-PRO-LYS-SHPHE-ALA-PRO WHEREIN N IS AS DEFINED ABOVE AND SHPE IS 3-AMINO-4 PHENYLBUTYRIC ACID, 9. A NONAPEPTIDE OF THE FORMULA PGLU-TRP-PRO-P-PRO-Q-ILE-PRO-PRO WHEREIN P IS ARG, HIS, LYS OR GLY AND Q IS GLN OR ASN, PGLU-TRP-PRO-R-PRO-S-T-ALA-PRO WHEREIN R IS ARG OR ORN, S IS NLE OR GLN AND T IS ILE OR PHE, PGLU-TRP-PRO-ORN-PRO-S-T-PRO-PRO WHEREIN S AND T ARE AS DEFINED ABOVE, PGLU-O-PRO-ARG-PRO-GLN-ILE-PRO-PRO WHEREIN O IS AS DEFINED ABOVE, PGLU-GLY-GLY-TRP-PRO-ARG-PRO-GLY-PRO-W-ILEPRO-PRO

Inventors

• 👤 M Ondetti
• 👤 J Pluscec

Bibliographic Details