1y91
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(New page: 200px<br /> <applet load="1y91" size="450" color="white" frame="true" align="right" spinBox="true" caption="1y91, resolution 2.15Å" /> '''Crystal structure o...)
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Revision as of 18:10, 12 November 2007
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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 with CT9 as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 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 Nov 12 20:16:33 2007
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. | CT9 | Atp-binding | Cdk2 | Cell cycle | Mitosis | Phosphorylation | Pyrazolopyrimidine inhibitor | Serine/threonine protein kinase
