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1p4f

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[[Image:1p4f.gif|left|200px]]
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{{Seed}}
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[[Image:1p4f.png|left|200px]]
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{{STRUCTURE_1p4f| PDB=1p4f | SCENE= }}
{{STRUCTURE_1p4f| PDB=1p4f | SCENE= }}
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'''DEATH ASSOCIATED PROTEIN KINASE CATALYTIC DOMAIN WITH BOUND INHIBITOR FRAGMENT'''
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===DEATH ASSOCIATED PROTEIN KINASE CATALYTIC DOMAIN WITH BOUND INHIBITOR FRAGMENT===
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==Overview==
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Death associated protein kinase (DAPK) is a calcium and calmodulin regulated enzyme that functions early in eukaryotic programmed cell death, or apoptosis. To validate DAPK as a potential drug discovery target for acute brain injury, the first small molecule DAPK inhibitor was synthesized and tested in vivo. A single injection of the aminopyridazine-based inhibitor administered 6 h after injury attenuated brain tissue or neuronal biomarker loss measured, respectively, 1 week and 3 days later. Because aminopyridazine is a privileged structure in neuropharmacology, we determined the high-resolution crystal structure of a binary complex between the kinase domain and a molecular fragment of the DAPK inhibitor. The co-crystal structure describes a structural basis for interaction and provides a firm foundation for structure-assisted design of lead compounds with appropriate molecular properties for future drug development.
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The line below this paragraph, {{ABSTRACT_PUBMED_14505650}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 14505650 is the PubMed ID number.
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{{ABSTRACT_PUBMED_14505650}}
==About this Structure==
==About this Structure==
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[[Category: Kinase]]
[[Category: Kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:40:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 00:16:52 2008''

Revision as of 21:16, 27 July 2008

Image:1p4f.png

Template:STRUCTURE 1p4f

DEATH ASSOCIATED PROTEIN KINASE CATALYTIC DOMAIN WITH BOUND INHIBITOR FRAGMENT

Template:ABSTRACT PUBMED 14505650

About this Structure

1P4F is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury., Velentza AV, Wainwright MS, Zasadzki M, Mirzoeva S, Schumacher AM, Haiech J, Focia PJ, Egli M, Watterson DM, Bioorg Med Chem Lett. 2003 Oct 20;13(20):3465-70. PMID:14505650

Page seeded by OCA on Mon Jul 28 00:16:52 2008

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