1wzy: Difference between revisions
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'''Crystal structure of human ERK2 complexed with a pyrazolopyridazine derivative'''<br /> | '''Crystal structure of human ERK2 complexed with a pyrazolopyridazine derivative'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
1WZY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with F29 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http:// | 1WZY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=F29:'>F29</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WZY OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: kinase]] | [[Category: kinase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 17:08:05 2008'' | ||
Revision as of 18:08, 15 February 2008
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Crystal structure of human ERK2 complexed with a pyrazolopyridazine derivative
OverviewOverview
A series of pyrazolopyridazine compounds were briefly investigated as ERK2, inhibitors. The crystal structure of ERK2 complexed with an allyl, derivative was determined. The compound induces structural change, including movement of the glycine-rich loop and peptide flip between, Met108-Glu109. As a result, the newly formed subsite can recognize small, hydrophobic substituents but not hydrophilic ones.
DiseaseDisease
Known diseases associated with this structure: Epileptic encephalopathy, Lennox-Gastaut type OMIM:[602897]
About this StructureAbout this Structure
1WZY is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
ReferenceReference
Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative., Kinoshita T, Warizaya M, Ohori M, Sato K, Neya M, Fujii T, Bioorg Med Chem Lett. 2006 Jan 1;16(1):55-8. Epub 2005 Oct 18. PMID:16242327
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