1y91
From Proteopedia
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|SITE= | |SITE= | ||
|LIGAND= <scene name='pdbligand=CT9:4-[5-(TRANS-4-AMINOCYCLOHEXYLAMINO)-3-ISOPROPYLPYRAZOLO[1,5-A]PYRIMIDIN-7-YLAMINO]-N,N-DIMETHYLBENZENESULFONAMIDE'>CT9</scene> | |LIGAND= <scene name='pdbligand=CT9:4-[5-(TRANS-4-AMINOCYCLOHEXYLAMINO)-3-ISOPROPYLPYRAZOLO[1,5-A]PYRIMIDIN-7-YLAMINO]-N,N-DIMETHYLBENZENESULFONAMIDE'>CT9</scene> | ||
| - | |ACTIVITY= [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] | + | |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= CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1y8y|1Y8Y]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1y91 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1y91 OCA], [http://www.ebi.ac.uk/pdbsum/1y91 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1y91 RCSB]</span> | ||
}} | }} | ||
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[[Category: Torrance, C J.]] | [[Category: Torrance, C J.]] | ||
[[Category: Williamson, D S.]] | [[Category: Williamson, D S.]] | ||
| - | [[Category: CT9]] | ||
[[Category: atp-binding]] | [[Category: atp-binding]] | ||
[[Category: cdk2]] | [[Category: cdk2]] | ||
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[[Category: serine/threonine protein kinase]] | [[Category: serine/threonine protein kinase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:00:19 2008'' |
Revision as of 22:00, 30 March 2008
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| , resolution 2.15Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | CDK2 (Homo sapiens) | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Related: | 1Y8Y
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal structure of human CDK2 complexed with a pyrazolo[1,5-a]pyrimidine inhibitor
Overview
The protein structure guided design of a series of pyrazolo[1,5-a]pyrimidines with high potency for human cyclin-dependent kinase 2 (CDK2) is described. Some examples were shown to inhibit the growth of human colon tumour cells, were equipotent for CDK1 and were selective against GSK-3beta and other kinases.
About this Structure
1Y91 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2., Williamson DS, Parratt MJ, Bower JF, Moore JD, Richardson CM, Dokurno P, Cansfield AD, Francis GL, Hebdon RJ, Howes R, Jackson PS, Lockie AM, Murray JB, Nunns CL, Powles J, Robertson A, Surgenor AE, Torrance CJ, Bioorg Med Chem Lett. 2005 Feb 15;15(4):863-7. PMID:15686876
Page seeded by OCA on Mon Mar 31 01:00:19 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Bower, J F. | Cansfield, A D. | Dokurno, P. | Francis, G L. | Hebdon, R J. | Howes, R. | Jackson, P S. | Lockie, A M. | Moore, J D. | Murray, J B. | Nunns, C L. | Parratt, M J. | Powles, J. | Richardson, C M. | Robertson, A. | Surgenor, A E. | Torrance, C J. | Williamson, D S. | Atp-binding | Cdk2 | Cell cycle | Mitosis | Phosphorylation | Pyrazolopyrimidine inhibitor | Serine/threonine protein kinase
