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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
3
|
| pubmed:dateCreated |
1993-12-3
|
| pubmed:abstractText |
One hundred Suc-X-Y-Ala-pNA peptides: (Suc: succinyl, pNA: p-nitroanilide, X, Y: Gly, Ala, Val, Leu, Ile, Phe, Pro, alpha-aminobutyric acid, norvaline, norleucine) were synthesized and their reaction constants with porcine pancreatic elastase (Km, kcat and kcat/Km) were determined. These reaction constants were quantitatively analyzed using the Free-Wilson/Fujita-Ban method. The contribution of amino acid side chains to the reaction constants Km, kcat and kcat/Km, expressed logarithmically, was found to be additive. On the other hand, 19 elastase inhibitors of the general formula CF3CO-X-Y-Ala-pNA (X,Y: ten amino acids) were synthesized, and their inhibition constants were compared with the Michaelis constant for the corresponding substrates and analyzed using free-energy-related substituent constants. In the analysis of amino acid side chains in the Y position, the Ki value of the inhibitor was generally correlated to the Km value of the substrate, which corresponded to the inhibitor, thus confirming the validity of the equation. log(1/Ki) = 1.271 log(1/Km) + 4.831 This study may serve as a prototypical approach to unraveling structure-activity relationships of peptide substrates and inhibitors of medicinal or agricultural importance.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Sep
|
| pubmed:issn |
0367-8377
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
42
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
216-26
|
| pubmed:dateRevised |
2000-12-18
|
| pubmed:meshHeading |
pubmed-meshheading:8225776-Amino Acid Sequence,
pubmed-meshheading:8225776-Kinetics,
pubmed-meshheading:8225776-Molecular Sequence Data,
pubmed-meshheading:8225776-Pancreatic Elastase,
pubmed-meshheading:8225776-Peptides,
pubmed-meshheading:8225776-Structure-Activity Relationship,
pubmed-meshheading:8225776-Substrate Specificity,
pubmed-meshheading:8225776-Trifluoroacetic Acid
|
| pubmed:year |
1993
|
| pubmed:articleTitle |
Quantitative structure-activity relationship (QSAR) study of elastase substrates and inhibitors.
|
| pubmed:affiliation |
Pharmaceutical Laboratory, Kirin Brewery Co. Ltd., Gunma, Japan.
|
| pubmed:publicationType |
Journal Article
|