1h07
From Proteopedia
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|PDB= 1h07 |SIZE=350|CAPTION= <scene name='initialview01'>1h07</scene>, resolution 1.85Å | |PDB= 1h07 |SIZE=350|CAPTION= <scene name='initialview01'>1h07</scene>, resolution 1.85Å | ||
|SITE= <scene name='pdbsite=MFP:Mfq+Binding+Site+For+Chain+A'>MFP</scene> | |SITE= <scene name='pdbsite=MFP:Mfq+Binding+Site+For+Chain+A'>MFP</scene> | ||
| - | |LIGAND= <scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene> | + | |LIGAND= <scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=MFP:((2-BROMO-4-METHYLPHENYL){6-[(4-{[(2R)-3-(DIMETHYLAMINO)-2-HYDROXYPROPYL]OXY}PHENYL)AMINO]PYRIMIDIN-4-YL}AMINO)ACETONITRILE'>MFP</scene>, <scene name='pdbligand=MFQ:((2-BROMO-4-METHYLPHENYL){6-[(4-{[(2S)-3-(DIMETHYLAMINO)-2-HYDROXYPROPYL]OXY}PHENYL)AMINO]PYRIMIDIN-4-YL}AMINO)ACETONITRILE'>MFQ</scene> |
| - | |ACTIVITY= [http://en.wikipedia.org/wiki/ | + | |ACTIVITY= <span class='plainlinks'>[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] </span> |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1h07 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1h07 OCA], [http://www.ebi.ac.uk/pdbsum/1h07 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1h07 RCSB]</span> | ||
}} | }} | ||
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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:[http://www.ncbi.nlm.nih.gov/pubmed/12941311 12941311] | 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:[http://www.ncbi.nlm.nih.gov/pubmed/12941311 12941311] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| + | [[Category: Non-specific serine/threonine protein kinase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Transferred entry: 2 7.11 1]] | ||
[[Category: Beattie, J F.]] | [[Category: Beattie, J F.]] | ||
[[Category: Breault, G A.]] | [[Category: Breault, G A.]] | ||
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[[Category: Pease, J E.]] | [[Category: Pease, J E.]] | ||
[[Category: Tucker, J A.]] | [[Category: Tucker, J A.]] | ||
| - | + | [[Category: serine/threonine-protein kinase,mitosis,transferase]] | |
| - | + | ||
| - | + | ||
| - | [[Category: serine/threonine-protein kinase | + | |
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| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:54:59 2008'' |
Revision as of 17:55, 30 March 2008
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| , resolution 1.85Å | |||||||
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| Sites: | |||||||
| Ligands: | , , | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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 Mar 30 20:54:59 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | 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. | Serine/threonine-protein kinase,mitosis,transferase
