[Synthesis and biological activity of analogs of a nonapeptide inhibitor of peptidyldipeptidase].
The synthesis of 5 analogues of the effective inhibitor of peptidyl dipeptidase, teprotide, has been carried out. The inhibitory and bradykinin-potentiating activity of these compounds has been assayed. N-Terminal pyroglutamic acid and positive charge of arginine in position 4 were found to be essential for biological activity of the inhibitor.
Filatova
M P
MP
Krit
N A
NA
Beschastnaia
N V
NV
Blokhina
A V
AV
Kozlova
N I
NI
D000595:Amino Acid Sequence; D000806:Angiotensin-Converting Enzyme Inhibitors; D000818:Animals; D001920:Bradykinin / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D002942:Circular Dichroism; D004357:Drug Synergism; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009842:Oligopeptides / Q000138:chemical synthesis*; D011487:Protein Conformation; D013722:Teprotide / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology
D000806:Angiotensin-Converting Enzyme Inhibitors; D009842:Oligopeptides; D013722:Teprotide; D001920:Bradykinin
Sintez i biologicheskaia aktivnost' analogov nonapeptidnogo ingibitora peptidildipeptidazy.