2ds1
From Proteopedia
(New page: 200px<br /> <applet load="2ds1" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ds1, resolution 2.0Å" /> '''Human cyclin depende...) |
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| - | [[Image:2ds1. | + | [[Image:2ds1.jpg|left|200px]]<br /><applet load="2ds1" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2ds1" size=" | + | |
caption="2ds1, resolution 2.0Å" /> | caption="2ds1, resolution 2.0Å" /> | ||
'''Human cyclin dependent kinase 2 complexed with the CDK4 inhibitor'''<br /> | '''Human cyclin dependent kinase 2 complexed with the CDK4 inhibitor'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2DS1 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 1CD as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] Full crystallographic information is available from [http:// | + | 2DS1 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=1CD:'>1CD</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2DS1 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: protein kinase]] | [[Category: protein kinase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:48:18 2008'' |
Revision as of 12:48, 23 January 2008
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Human cyclin dependent kinase 2 complexed with the CDK4 inhibitor
Overview
The design of a novel series of cyclin-dependent kinase (CDK) inhibitors, containing a macrocyclic quinoxaline-2-one is reported. Structure-based, drug design and optimization from the starting point of diarylurea 2, which we previously reported as a moderate CDK1,2,4,6 inhibitor [J., Biol.Chem.2001, 276, 27548], led to the discovery of potent CDK1,2,4,6, inhibitor that were suitable for iv administration for in vivo study.
About this Structure
2DS1 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Cyclin-dependent kinase, with EC number 2.7.11.22 Full crystallographic information is available from OCA.
Reference
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure., Kawanishi N, Sugimoto T, Shibata J, Nakamura K, Masutani K, Ikuta M, Hirai H, Bioorg Med Chem Lett. 2006 Oct 1;16(19):5122-6. Epub 2006 Jul 28. PMID:16876403
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