This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


1eat

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:1eat.gif|left|200px]]
+
{{Seed}}
 +
[[Image:1eat.png|left|200px]]
<!--
<!--
Line 9: Line 10:
{{STRUCTURE_1eat| PDB=1eat | SCENE= }}
{{STRUCTURE_1eat| PDB=1eat | SCENE= }}
-
'''NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 5. DESIGN, SYNTHESIS, AND X-RAY CRYSTALLOGRAPHY OF A SERIES OF ORALLY ACTIVE 5-AMINO-PYRIMIDIN-6-ONE-CONTAINING TRIFLUOROMETHYLKETONES'''
+
===NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 5. DESIGN, SYNTHESIS, AND X-RAY CRYSTALLOGRAPHY OF A SERIES OF ORALLY ACTIVE 5-AMINO-PYRIMIDIN-6-ONE-CONTAINING TRIFLUOROMETHYLKETONES===
-
==Overview==
+
<!--
-
The effects of changes in substitution in a series of 5-amino-2-pyrimidin-6-ones on both in vitro activity and oral activity in an acute hemorrhagic assay have been explored. These compounds contained either a trifluoromethyl ketone or a boronic acid moiety to bind covalently to the Ser-195 hydroxyl of human leukocyte elastase (HLE). Boronic acid-containing inhibitors were found to be more potent than the corresponding trifluoromethyl ketones in vitro but were less active upon oral administration. Compound 13b was found to offer the best combination of oral potency, duration of action, and enzyme selectivity and, as such, was selected for further biological testing. X-ray crystallography of a cocrystallized complex of compound 19m and porcine pancreatic elastase demonstrated that the inhibitor is bound to the enzyme in a manner similar to that found previously for a closely related series of pyridone-containing inhibitors of HLE.
+
The line below this paragraph, {{ABSTRACT_PUBMED_7837246}}, adds the Publication Abstract to the page
 +
(as it appears on PubMed at http://www.pubmed.gov), where 7837246 is the PubMed ID number.
 +
-->
 +
{{ABSTRACT_PUBMED_7837246}}
==About this Structure==
==About this Structure==
Line 24: Line 28:
[[Category: Sus scrofa]]
[[Category: Sus scrofa]]
[[Category: Ceccarelli, C.]]
[[Category: Ceccarelli, C.]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 14:52:56 2008''
+
 
 +
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 00:25:28 2008''

Revision as of 21:25, 30 June 2008

Image:1eat.png

Template:STRUCTURE 1eat

NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 5. DESIGN, SYNTHESIS, AND X-RAY CRYSTALLOGRAPHY OF A SERIES OF ORALLY ACTIVE 5-AMINO-PYRIMIDIN-6-ONE-CONTAINING TRIFLUOROMETHYLKETONES

Template:ABSTRACT PUBMED 7837246

About this Structure

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

Reference

Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethyl ketones., Veale CA, Bernstein PR, Bryant C, Ceccarelli C, Damewood JR Jr, Earley R, Feeney SW, Gomes B, Kosmider BJ, Steelman GB, et al., J Med Chem. 1995 Jan 6;38(1):98-108. PMID:7837246

Page seeded by OCA on Tue Jul 1 00:25:28 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1eat"
Personal tools