1wzy: Difference between revisions

Revision as of 14:21, 3 May 2008

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.

About this StructureAbout this Structure

1WZY is a Single protein structure of sequence from Homo sapiens. 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 Page seeded by OCA on Sat May 3 14:21:38 2008

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

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 [[Image:1wzy.jpg|left|200px]]
- {{Structure
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+The line below this paragraph, containing "STRUCTURE_1wzy", creates the "Structure Box" on the page.
-|SITE=
+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=F29:1-ALLYL-5-(2-PHENYLPYRAZOLO[1,5-A]PYRIDIN-3-YL)-1H-PYRAZOLO[3,4-C]PYRIDAZIN-3-AMINE'>F29</scene>
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-|ACTIVITY= <span class='plainlinks'>[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] </span>
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-}}
 '''Crystal structure of human ERK2 complexed with a pyrazolopyridazine derivative'''
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 [[Category: Single protein]]
 [[Category: Kinoshita, T.]]
-[[Category: erk2]]
+[[Category: Erk2]]
-[[Category: inhibitor]]
+[[Category: Inhibitor]]
-[[Category: kinase]]
+[[Category: Kinase]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 14:21:38 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:43:09 2008''