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Volumn 9, Issue 3, 1999, Pages 413-418

Symmetrical anhydride-type serine protease inhibitors: Structure- activity relationship studies of human chymase inhibitors

Author keywords

[No Author keywords available]

Indexed keywords

ACID ANHYDRIDE; CHYMASE; CHYMASE INHIBITOR; SERINE PROTEINASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 0033535116     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00012-8     Document Type: Article
Times cited : (27)

References (16)
  • 12
    • 0013588527 scopus 로고    scopus 로고
    • note
    • Enzyme assay; The inhibitory effects of each compound on the enzymatic activities of five serine proteases were evaluated using the purified enzymes and chromogenic substrates. The enzymes and those substrates used here were as follow, N-succinyl-Ala-Ala-Pro-Phe-pNA (1.5 mM) for human recombinant chymase and bovine pancreatic α-chymotrypsin (Sigma Type I-S; 47 ng/mL); N-succinyl-Ala-Ala-Pro-Phe-pNA (3 mM) for human leukocyte cathepsin G (Elastin Products Co., Inc.; 2.5 U/mL); N-succinyl-Ala-Ala-Ala- pNA (1 mM) for porcine pancreatic elastase (Sigma Type III; 0.8 mg/mL); Bz-L-Arg-pNA (1 mM) for porcine pancreatic trypsin (Wako Pure Chemicals; 1 U/mL). All experiments were carried out using 50 mM HEPES buffer (pH 7.4) containing 0.1 mM NaCl, except for the buffer used for chymase, which contained 50 mM Tris-HCl (pH 8.0) and 1 M KCl.
  • 13
    • 0013617749 scopus 로고    scopus 로고
    • note
    • Each enantiomer of 2,2-dimemyl-3-(N-benzoyl)amino-5-phenylpentanoic acid was isolated by HPLC using chiral column (CHIRALCEL OD, 10 × 250 mm) eluted with a mixture of hexane and 2-propanol (3:1) and was used for the anhydride formation according to the procedure shown in Scheme 1.
  • 14
    • 0013590717 scopus 로고    scopus 로고
    • note
    • D = +51.0° (c 0.25, MeOH).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.