Title of article
The crystal structure of the complex of non-peptidic inhibitor of human neutrophil elastase ONO-6818 and porcine pancreatic elastase Original Research Article
Author/Authors
Y Odagaki، نويسنده , , K Ohmoto، نويسنده , , S Matsuoka، نويسنده , , N Hamanaka، نويسنده , , H Nakai، نويسنده , , M Toda، نويسنده , , Y Katsuya، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
5
From page
647
To page
651
Abstract
The crystal structure of a new inhibitor of human neutrophil elastase (HNE), N-[2-[5-(tert-butyl)-1,3,4-oxadiazol-2-yl]-(1RS)-1-(methylethyl)-2-oxoethyl]-2-(5-amino-6-oxo-2-phenyl-6H-pyrimidin-1-ly)acetamide (ONO-6818, 1) complexed to porcine pancreatic elastase (PPE) has been determined at 1.86 Å resolution. Analytical results provided evidence of a 1:1 complex in which the electrophilic ketone of 1 covalently bound to Oγ of Ser195 at the active site of PPE. The role of the unique electron-withdrawing ketone of 1 has been elucidated.
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2001
Journal title
Bioorganic and Medicinal Chemistry
Record number
1301407
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