Document Detail


Synthesis of a trihexacontapeptide corresponding to the sequence 8-70 of eglin c and studies on the relationship between the structure and the inhibitory activity against human leukocyte elastase, cathepsin G and alpha-chymotrypsin.
MedLine Citation:
PMID:  2226822     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A trihexacontapeptide corresponding to the sequence 8-70 of eglin c and its related peptides were synthesized by the conventional solution method and their inhibitory activity against human leukocyte elastase, cathepsin G and alpha-chymotrypsin was examined. Although synthetic eglin c (41-49) inhibited cathepsin G and alpha-chymotrypsin (Ki = 4.0 x 10(-5) M and 2.0 x 10(-5) M, respectively) but not leukocyte elastase, the synthetic trihexacontapeptide potently inhibited cathepsin G, alpha-chymotrypsin and leukocyte elastase (Ki = 1.8 x 10(-9) M, 1.4 x 10(-9) M and 2.2 x 10(-9) M, respectively). The relationship between the structure of eglin c and the inhibitory activity against the above enzymes is also described.
Authors:
Y Okada; S Tsuboi; Y Tsuda; Y Nagamatsu; J Yamamoto
Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  FEBS letters     Volume:  272     ISSN:  0014-5793     ISO Abbreviation:  FEBS Lett.     Publication Date:  1990 Oct 
Date Detail:
Created Date:  1990-12-13     Completed Date:  1990-12-13     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  0155157     Medline TA:  FEBS Lett     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  113-6     Citation Subset:  IM    
Affiliation:
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.
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MeSH Terms
Descriptor/Qualifier:
Amino Acid Sequence
Cathepsin G
Cathepsins / antagonists & inhibitors*
Chymotrypsin / antagonists & inhibitors*
Electrochemistry
Humans
Hydrogen Bonding
Leukocyte Elastase
Molecular Sequence Data
Pancreatic Elastase / antagonists & inhibitors*
Peptide Fragments / chemical synthesis*,  chemistry,  pharmacology
Proteins
Serine Endopeptidases
Serine Proteinase Inhibitors / chemistry*
Serpins*
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Peptide Fragments; 0/Proteins; 0/Serine Proteinase Inhibitors; 0/Serpins; 0/eglin proteinase inhibitors; EC 3.4.-/Cathepsins; EC 3.4.21.-/Serine Endopeptidases; EC 3.4.21.1/Chymotrypsin; EC 3.4.21.20/CTSG protein, human; EC 3.4.21.20/Cathepsin G; EC 3.4.21.36/Pancreatic Elastase; EC 3.4.21.37/Leukocyte Elastase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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