2b52
From Proteopedia
(New page: 200px<br /> <applet load="2b52" size="450" color="white" frame="true" align="right" spinBox="true" caption="2b52, resolution 1.88Å" /> '''Human cyclin depend...) |
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| - | [[Image:2b52.gif|left|200px]]<br /> | + | [[Image:2b52.gif|left|200px]]<br /><applet load="2b52" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2b52" size=" | + | |
caption="2b52, resolution 1.88Å" /> | caption="2b52, resolution 1.88Å" /> | ||
'''Human cyclin dependent kinase 2 (CDK2) complexed with DPH-042562'''<br /> | '''Human cyclin dependent kinase 2 (CDK2) complexed with DPH-042562'''<br /> | ||
==Overview== | ==Overview== | ||
| - | New indeno[1,2-c]pyrazol-4-one cyclin dependent kinase inhibitors have | + | New indeno[1,2-c]pyrazol-4-one cyclin dependent kinase inhibitors have been disclosed. The most promising compounds are nanomolar enzyme inhibitors with excellent activity against tumor cells. The most advanced compound retains cell culture activity even in the presence of human serum proteins. The most advanced compound did not kill the normal fibroblast line AG1523. |
==About this Structure== | ==About this Structure== | ||
| - | 2B52 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 D42 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:// | + | 2B52 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=D42:'>D42</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=2B52 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 16:34:14 2008'' |
Revision as of 14:34, 21 February 2008
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Human cyclin dependent kinase 2 (CDK2) complexed with DPH-042562
Overview
New indeno[1,2-c]pyrazol-4-one cyclin dependent kinase inhibitors have been disclosed. The most promising compounds are nanomolar enzyme inhibitors with excellent activity against tumor cells. The most advanced compound retains cell culture activity even in the presence of human serum proteins. The most advanced compound did not kill the normal fibroblast line AG1523.
About this Structure
2B52 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
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3., Yue EW, DiMeo SV, Higley CA, Markwalder JA, Burton CR, Benfield PA, Grafstrom RH, Cox S, Muckelbauer JK, Smallwood AM, Chen H, Chang CH, Trainor GL, Seitz SP, Bioorg Med Chem Lett. 2004 Jan 19;14(2):343-6. PMID:14698155
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