2c6m
From Proteopedia
(New page: 200px<br /> <applet load="2c6m" size="450" color="white" frame="true" align="right" spinBox="true" caption="2c6m, resolution 1.90Å" /> '''CRYSTAL STRUCTURE O...) |
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==About this Structure== | ==About this Structure== | ||
| - | 2C6M 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 DT5 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=2C6M OCA]]. | + | 2C6M 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 DT5 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: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C6M OCA]]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| + | [[Category: Transferred entry: 2.7.11.1]] | ||
[[Category: Dokurno, P.]] | [[Category: Dokurno, P.]] | ||
[[Category: Murray, J.B.]] | [[Category: Murray, J.B.]] | ||
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[[Category: triazolopyrimidine inhibitor]] | [[Category: triazolopyrimidine inhibitor]] | ||
| - | ''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 11:27:54 2007'' |
Revision as of 09:23, 30 October 2007
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CRYSTAL STRUCTURE OF THE HUMAN CDK2 COMPLEXED WITH THE TRIAZOLOPYRIMIDINE INHIBITOR
Overview
Crystallographic and modelling data, in conjunction with a medicinal, chemistry template-hopping approach, led to the identification of a series, of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3beta (GSK-3beta). One, example had a CDK2 IC(50) of 120 nM and showed selectivity over GSK-3beta, of 167-fold.
About this Structure
2C6M is a [Single protein] structure of sequence from [Homo sapiens] with DT5 as [ligand]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
Reference
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR., Richardson CM, Williamson DS, Parratt MJ, Borgognoni J, Cansfield AD, Dokurno P, Francis GL, Howes R, Moore JD, Murray JB, Robertson A, Surgenor AE, Torrance CJ, Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. Epub 2005 Dec 1. PMID:16325401
Page seeded by OCA on Tue Oct 30 11:27:54 2007
Categories: Homo sapiens | Single protein | Transferred entry: 2.7.11.1 | Dokurno, P. | Murray, J.B. | Richardson, C.M. | Surgenor, A.E. | DT5 | Atp-binding | Cdk2 | Cell cycle | Cell division | Kinase | Mitosis | Nucleotide-binding | Phosphorylation | Polymorphism | Serine/threonine protein kinase | Transferase | Triazolopyrimidine inhibitor
