1y91
From Proteopedia
(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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| - | [[Image:1y91.gif|left|200px]]<br /> | + | [[Image:1y91.gif|left|200px]]<br /><applet load="1y91" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1y91" size=" | + | |
caption="1y91, resolution 2.15Å" /> | caption="1y91, resolution 2.15Å" /> | ||
'''Crystal structure of human CDK2 complexed with a pyrazolo[1,5-a]pyrimidine inhibitor'''<br /> | '''Crystal structure of human CDK2 complexed with a pyrazolo[1,5-a]pyrimidine inhibitor'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The protein structure guided design of a series of | + | 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== | ==About this Structure== | ||
| - | 1Y91 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 CT9 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http:// | + | 1Y91 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=CT9:'>CT9</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Y91 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Bower, J | + | [[Category: Bower, J F.]] |
| - | [[Category: Cansfield, A | + | [[Category: Cansfield, A D.]] |
[[Category: Dokurno, P.]] | [[Category: Dokurno, P.]] | ||
| - | [[Category: Francis, G | + | [[Category: Francis, G L.]] |
| - | [[Category: Hebdon, R | + | [[Category: Hebdon, R J.]] |
[[Category: Howes, R.]] | [[Category: Howes, R.]] | ||
| - | [[Category: Jackson, P | + | [[Category: Jackson, P S.]] |
| - | [[Category: Lockie, A | + | [[Category: Lockie, A M.]] |
| - | [[Category: Moore, J | + | [[Category: Moore, J D.]] |
| - | [[Category: Murray, J | + | [[Category: Murray, J B.]] |
| - | [[Category: Nunns, C | + | [[Category: Nunns, C L.]] |
| - | [[Category: Parratt, M | + | [[Category: Parratt, M J.]] |
[[Category: Powles, J.]] | [[Category: Powles, J.]] | ||
| - | [[Category: Richardson, C | + | [[Category: Richardson, C M.]] |
[[Category: Robertson, A.]] | [[Category: Robertson, A.]] | ||
| - | [[Category: Surgenor, A | + | [[Category: Surgenor, A E.]] |
| - | [[Category: Torrance, C | + | [[Category: Torrance, C J.]] |
| - | [[Category: Williamson, D | + | [[Category: Williamson, D S.]] |
[[Category: CT9]] | [[Category: CT9]] | ||
[[Category: atp-binding]] | [[Category: atp-binding]] | ||
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[[Category: serine/threonine protein kinase]] | [[Category: serine/threonine protein kinase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:02:56 2008'' |
Revision as of 14:02, 21 February 2008
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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 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 Thu Feb 21 16:02:56 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. | CT9 | Atp-binding | Cdk2 | Cell cycle | Mitosis | Phosphorylation | Pyrazolopyrimidine inhibitor | Serine/threonine protein kinase
