1h07
From Proteopedia
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==Overview== | ==Overview== | ||
- | Using a high-throughput screening campaign, we identified the 4,6-bis | + | 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== | ==About this Structure== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
- | [[Category: Transferred entry: 2 | + | [[Category: Transferred entry: 2 7.11 1]] |
- | [[Category: Beattie, J | + | [[Category: Beattie, J F.]] |
- | [[Category: Breault, G | + | [[Category: Breault, G A.]] |
- | [[Category: Ellston, R | + | [[Category: Ellston, R P.A.]] |
[[Category: Green, S.]] | [[Category: Green, S.]] | ||
- | [[Category: Jewsbury, P | + | [[Category: Jewsbury, P J.]] |
- | [[Category: Midgley, C | + | [[Category: Midgley, C J.]] |
- | [[Category: Minshull, C | + | [[Category: Minshull, C A.]] |
- | [[Category: Naven, R | + | [[Category: Naven, R T.]] |
- | [[Category: Pauptit, R | + | [[Category: Pauptit, R A.]] |
- | [[Category: Pease, J | + | [[Category: Pease, J E.]] |
- | [[Category: Tucker, J | + | [[Category: Tucker, J A.]] |
[[Category: ACE]] | [[Category: ACE]] | ||
[[Category: MFP]] | [[Category: MFP]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:55:56 2008'' |
Revision as of 10:55, 21 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
1H07 is a Single protein structure of sequence from Homo sapiens with and as ligands. 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 Thu Feb 21 12:55:56 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. | ACE | MFP | Mitosis | Serine/threonine-protein kinase | Transferase