1x8b
From Proteopedia
(New page: 200px<br /> <applet load="1x8b" size="450" color="white" frame="true" align="right" spinBox="true" caption="1x8b, resolution 1.81Å" /> '''Structure of human ...) |
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| - | [[Image:1x8b.gif|left|200px]]<br /> | + | [[Image:1x8b.gif|left|200px]]<br /><applet load="1x8b" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1x8b, resolution 1.81Å" /> | caption="1x8b, resolution 1.81Å" /> | ||
'''Structure of human Wee1A kinase: kinase domain complexed with inhibitor PD0407824'''<br /> | '''Structure of human Wee1A kinase: kinase domain complexed with inhibitor PD0407824'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Phosphorylation is critical to regulation of the eukaryotic cell cycle. | + | Phosphorylation is critical to regulation of the eukaryotic cell cycle. Entry to mitosis is triggered by the cyclin-dependent kinase CDK1 (Cdc2), which is inactivated during the preceding S and G2 phases by phosphorylation of T14 and Y15. Two homologous kinases, Wee1, which phosphorylates Y15, and Myt1, which phosphorylates both T14 and Y15, mediate this inactivation. We have determined the crystal structure of the catalytic domain of human somatic Wee1 (Wee1A) complexed with an active-site inhibitor at 1.8 A resolution. Although Wee1A is functionally a tyrosine kinase, in sequence and structure it most closely resembles serine/threonine kinases such as Chk1 and cAMP kinases. The crystal structure shows that although the catalytic site closely resembles that of other protein kinases, the activation segment contains Wee1-specific features that maintain it in an active conformation and, together with a key substitution in its glycine-rich loop, help determine its substrate specificity. |
==About this Structure== | ==About this Structure== | ||
| - | 1X8B 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 MG and 824 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] Full crystallographic information is available from [http:// | + | 1X8B 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=MG:'>MG</scene> and <scene name='pdbligand=824:'>824</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1X8B OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Transferase]] | [[Category: Transferase]] | ||
| - | [[Category: Baker, E | + | [[Category: Baker, E N.]] |
| - | [[Category: Dickson, J | + | [[Category: Dickson, J M.]] |
[[Category: Ivanovic, I.]] | [[Category: Ivanovic, I.]] | ||
| - | [[Category: Squire, C | + | [[Category: Squire, C J.]] |
[[Category: 824]] | [[Category: 824]] | ||
[[Category: MG]] | [[Category: MG]] | ||
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[[Category: wee1]] | [[Category: wee1]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:52:01 2008'' |
Revision as of 13:52, 21 February 2008
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Structure of human Wee1A kinase: kinase domain complexed with inhibitor PD0407824
Overview
Phosphorylation is critical to regulation of the eukaryotic cell cycle. Entry to mitosis is triggered by the cyclin-dependent kinase CDK1 (Cdc2), which is inactivated during the preceding S and G2 phases by phosphorylation of T14 and Y15. Two homologous kinases, Wee1, which phosphorylates Y15, and Myt1, which phosphorylates both T14 and Y15, mediate this inactivation. We have determined the crystal structure of the catalytic domain of human somatic Wee1 (Wee1A) complexed with an active-site inhibitor at 1.8 A resolution. Although Wee1A is functionally a tyrosine kinase, in sequence and structure it most closely resembles serine/threonine kinases such as Chk1 and cAMP kinases. The crystal structure shows that although the catalytic site closely resembles that of other protein kinases, the activation segment contains Wee1-specific features that maintain it in an active conformation and, together with a key substitution in its glycine-rich loop, help determine its substrate specificity.
About this Structure
1X8B is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 Full crystallographic information is available from OCA.
Reference
Structure and inhibition of the human cell cycle checkpoint kinase, Wee1A kinase: an atypical tyrosine kinase with a key role in CDK1 regulation., Squire CJ, Dickson JM, Ivanovic I, Baker EN, Structure. 2005 Apr;13(4):541-50. PMID:15837193
Page seeded by OCA on Thu Feb 21 15:52:01 2008
Categories: Homo sapiens | Single protein | Transferase | Baker, E N. | Dickson, J M. | Ivanovic, I. | Squire, C J. | 824 | MG | Cell cycle | Kinase | Wee1
