1v1k
From Proteopedia
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| - | [[Image:1v1k.gif|left|200px]]<br /><applet load="1v1k" size=" | + | [[Image:1v1k.gif|left|200px]]<br /><applet load="1v1k" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1v1k, resolution 2.31Å" /> | caption="1v1k, resolution 2.31Å" /> | ||
'''CDK2 IN COMPLEX WITH A DISUBSTITUTED 4, 6-BIS ANILINO PYRIMIDINE CDK4 INHIBITOR'''<br /> | '''CDK2 IN COMPLEX WITH A DISUBSTITUTED 4, 6-BIS ANILINO PYRIMIDINE CDK4 INHIBITOR'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1V1K 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 ACE and 3FP as [http://en.wikipedia.org/wiki/ligands ligands]. This structure superseeds the now removed PDB entry 1H06. 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] Known structural/functional Site: <scene name='pdbsite=AC1:3fp Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http:// | + | 1V1K 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=ACE:'>ACE</scene> and <scene name='pdbligand=3FP:'>3FP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. This structure superseeds the now removed PDB entry 1H06. 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] Known structural/functional Site: <scene name='pdbsite=AC1:3fp+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1V1K OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 10:16:48 2008'' |
Revision as of 08:16, 3 February 2008
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CDK2 IN COMPLEX WITH A DISUBSTITUTED 4, 6-BIS ANILINO PYRIMIDINE CDK4 INHIBITOR
Overview
Using a high-throughput screening campaign, we identified the 4,6-bis, anilino pyrimidines as inhibitors of the cyclin-dependent kinase, CDK4., Herein we describe the further chemical modification and use of X-ray, crystallography to develop potent and selective in vitro inhibitors of, CDK4.
About this Structure
1V1K is a Single protein structure of sequence from Homo sapiens with and as ligands. This structure superseeds the now removed PDB entry 1H06. Active as Transferred entry: 2.7.11.1, with EC number 2.7.1.37 Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines., Beattie JF, Breault GA, Ellston RP, Green S, Jewsbury PJ, Midgley CJ, Naven RT, Minshull CA, Pauptit RA, Tucker JA, Pease JE, Bioorg Med Chem Lett. 2003 Sep 15;13(18):2955-60. PMID:12941311
Page seeded by OCA on Sun Feb 3 10:16:48 2008
Categories: Homo sapiens | Single protein | Transferred entry: 2.7.11.1 | Beattie, J.F. | Breault, G.A. | Ellston, R.P.A. | Green, S. | Jewsbury, P.J. | Midgley, C.J. | Minshull, C.A. | Naven, R.T. | Pauptit, R.A. | Pease, J.E. | Tucker, J.A. | 3FP | ACE | Mitosis | Serine/threonine-protein kinase | Transferase
