Amino acids and peptides. XXX. Synthesis of eglin c (41-49) and eglin c (60-63) and examination of their inhibitory activity towards human leukocyte elastase, cathepsin G, porcine pancreatic elastase and alpha-chymotrypsin.
H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OH and H-Thr-Asn-Val-Val-OH, which correspond to the sequences 41-49 and 60-63 of eglin c, respectively, were synthesized by a conventional solution approach using the newly developed 6-chloro-2-pyridyl ester method. The inhibitory activities of the above two peptides against human leukocyte elastase, cathepsin G, porcine pancreatic elastase and alpha-chymotrypsin were examined in comparison with those of the corresponding methyl esters.
Tsuboi
S
S
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.
Takeda
M
M
Okada
Y
Y
Nagamatsu
Y
Y
Yamamoto
J
J
D000595:Amino Acid Sequence; D000596:Amino Acids / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D056649:Cathepsin G; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D002918:Chymotrypsin / Q000037:antagonists & inhibitors*; D006801:Humans; D007962:Leukocytes / Q000187:drug effects / Q000201:enzymology*; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D010179:Pancreas / Q000201:enzymology; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D012697:Serine Endopeptidases; D013552:Swine
D000596:Amino Acids; D009842:Oligopeptides; D010455:Peptides; C069313:eglin c (41-49); C069312:eglin c (60-63); D002403:Cathepsins; D012697:Serine Endopeptidases; D002918:Chymotrypsin; C534094:CTSG protein, human; D056649:Cathepsin G; D010196:Pancreatic Elastase