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1eau

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[[Image:1eau.jpg|left|200px]]
[[Image:1eau.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1eau |SIZE=350|CAPTION= <scene name='initialview01'>1eau</scene>, resolution 2.0&Aring;
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The line below this paragraph, containing "STRUCTURE_1eau", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=BDK:2-[5-AMINO-6-OXO-2-(2-THIENYL)-1,6-DIHYDROPYRIMIDIN-1-YL)-N-[3,3-DIFLUORO+-1-ISOPROPYL-2-OXO-3-(N-(2-MORPHOLINO+ETHYL)CARBAMOYL]PROPYL]ACETAMIDE'>BDK</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Pancreatic_elastase Pancreatic elastase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.36 3.4.21.36] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1eau| PDB=1eau | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1eau FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1eau OCA], [http://www.ebi.ac.uk/pdbsum/1eau PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1eau RCSB]</span>
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}}
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'''NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 6. DESIGN OF A POTENT, INTRATRACHEALLY ACTIVE, PYRIDONE-BASED TRIFLUOROMETHYL KETONE'''
'''NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 6. DESIGN OF A POTENT, INTRATRACHEALLY ACTIVE, PYRIDONE-BASED TRIFLUOROMETHYL KETONE'''
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[[Category: Sus scrofa]]
[[Category: Sus scrofa]]
[[Category: Ceccarelli, C.]]
[[Category: Ceccarelli, C.]]
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[[Category: hydrolase (serine protease)]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 14:53:05 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 19:58:54 2008''
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Revision as of 11:53, 2 May 2008

Image:1eau.jpg

Template:STRUCTURE 1eau

NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 6. DESIGN OF A POTENT, INTRATRACHEALLY ACTIVE, PYRIDONE-BASED TRIFLUOROMETHYL KETONE


Overview

Further modification of the 3-amino substituent in a trifluoromethyl ketone-based series of 3-amino-6-phenylpyridin-2-ones that had been optimized for oral activity led to analogs that were potent intratracheal inhibitors in a model of HLE-induced lung damage in the hamster. The best 3-amino substituent for intratracheal activity is [4-[N-[(4-chlorophenyl)sulfonyl]-carbamoyl]phenyl]sulfonyl. At a 30 min prechallenge interval, compound 9, which incorporates this substituent, had an ED50 of approximately 2 nmol/animal and, qualitatively, afforded a very similar dose-response relationship to that found with a peptidic trifluoromethyl ketone inhibitor, ICI 200,355.

About this Structure

1EAU is a Single protein structure of sequence from Sus scrofa. Full crystallographic information is available from OCA.

Reference

Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, intratracheally active, pyridone-based trifluoromethyl ketone., Bernstein PR, Gomes BC, Kosmider BJ, Vacek EP, Williams JC, J Med Chem. 1995 Jan 6;38(1):212-5. PMID:7837235 Page seeded by OCA on Fri May 2 14:53:05 2008

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