1e9h
From Proteopedia
(New page: 200px<br /> <applet load="1e9h" size="450" color="white" frame="true" align="right" spinBox="true" caption="1e9h, resolution 2.5Å" /> '''THR 160 PHOSPHORYLAT...) |
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==About this Structure== | ==About this Structure== | ||
| - | 1E9H is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with INR as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1E9H OCA]]. | + | 1E9H is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with INR as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]]. Structure known Active Site: INA. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1E9H OCA]]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| + | [[Category: Transferred entry: 2.7.11.1]] | ||
[[Category: Davies, T.G.]] | [[Category: Davies, T.G.]] | ||
[[Category: Endicott, J.A.]] | [[Category: Endicott, J.A.]] | ||
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[[Category: phosphorylation]] | [[Category: phosphorylation]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 11:50:05 2007'' |
Revision as of 09:45, 30 October 2007
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THR 160 PHOSPHORYLATED CDK2-HUMAN CYCLIN A3 COMPLEX WITH THE INHIBITOR INDIRUBIN-5-SULPHONATE BOUND
Overview
BACKGROUND: Cyclin-dependent kinase 2 (CDK2) is an important target for, structure-based design of antitumor agents. Monomeric CDK2 is inactive., Activation requires rearrangements to key structural elements of the, enzyme's active site, which accompany cyclin binding and phosphorylation., To assess the validity of using monomeric CDK2 as a model for the active, kinase in structure-based drug design, we have solved the structure of the, inhibitor indirubin-5-sulphonate (E226) complexed with phospho-CDK2-cyclin, A and compared it with the structure of E226 bound to inactive, monomeric, CDK2. RESULTS: Activation of monomeric CDK2 leads to a rotation of its, N-terminal domain relative to the C-terminal lobe. The accompanying change, in position of E226 follows that of the N-terminal domain, ... [(full description)]
About this Structure
1E9H is a [Protein complex] structure of sequences from [Homo sapiens] with INR as [ligand]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: INA. Full crystallographic information is available from [OCA].
Reference
Inhibitor binding to active and inactive CDK2: the crystal structure of CDK2-cyclin A/indirubin-5-sulphonate., Davies TG, Tunnah P, Meijer L, Marko D, Eisenbrand G, Endicott JA, Noble ME, Structure. 2001 May 9;9(5):389-97. PMID:11377199
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