2b53
From Proteopedia
(New page: 200px<br /> <applet load="2b53" size="450" color="white" frame="true" align="right" spinBox="true" caption="2b53, resolution 2.00Å" /> '''Human cyclin depend...) |
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| - | [[Image:2b53.gif|left|200px]]<br /> | + | [[Image:2b53.gif|left|200px]]<br /><applet load="2b53" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2b53" size=" | + | |
caption="2b53, resolution 2.00Å" /> | caption="2b53, resolution 2.00Å" /> | ||
'''Human cyclin dependent kinase 2 (CDK2) complexed with DIN-234325'''<br /> | '''Human cyclin dependent kinase 2 (CDK2) complexed with DIN-234325'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. | + | Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. Aspects of the SAR were investigated using solution-phase, parallel synthesis. An X-ray crystal structure was obtained of quinazoline 51 bound in CDK2 and key interactions within the ATP binding pocket are defined. |
==About this Structure== | ==About this Structure== | ||
| - | 2B53 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 D23 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:// | + | 2B53 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=D23:'>D23</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=2B53 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 Thu Feb 21 16:34:15 2008'' |
Revision as of 14:34, 21 February 2008
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Human cyclin dependent kinase 2 (CDK2) complexed with DIN-234325
Overview
Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. Aspects of the SAR were investigated using solution-phase, parallel synthesis. An X-ray crystal structure was obtained of quinazoline 51 bound in CDK2 and key interactions within the ATP binding pocket are defined.
About this Structure
2B53 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.
Reference
Quinazolines as cyclin dependent kinase inhibitors., Sielecki TM, Johnson TL, Liu J, Muckelbauer JK, Grafstrom RH, Cox S, Boylan J, Burton CR, Chen H, Smallwood A, Chang CH, Boisclair M, Benfield PA, Trainor GL, Seitz SP, Bioorg Med Chem Lett. 2001 May 7;11(9):1157-60. PMID:11354366
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