1y91

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[[Image:1y91.gif|left|200px]]
[[Image:1y91.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1y91 |SIZE=350|CAPTION= <scene name='initialview01'>1y91</scene>, resolution 2.15&Aring;
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The line below this paragraph, containing "STRUCTURE_1y91", creates the "Structure Box" on the page.
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|SITE=
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|LIGAND= <scene name='pdbligand=CT9:4-[5-(TRANS-4-AMINOCYCLOHEXYLAMINO)-3-ISOPROPYLPYRAZOLO[1,5-A]PYRIMIDIN-7-YLAMINO]-N,N-DIMETHYLBENZENESULFONAMIDE'>CT9</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|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>
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or leave the SCENE parameter empty for the default display.
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|GENE= CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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|DOMAIN=
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{{STRUCTURE_1y91| PDB=1y91 | SCENE= }}
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|RELATEDENTRY=[[1y8y|1Y8Y]]
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|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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}}
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'''Crystal structure of human CDK2 complexed with a pyrazolo[1,5-a]pyrimidine inhibitor'''
'''Crystal structure of human CDK2 complexed with a pyrazolo[1,5-a]pyrimidine inhibitor'''
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[[Category: Torrance, C J.]]
[[Category: Torrance, C J.]]
[[Category: Williamson, D S.]]
[[Category: Williamson, D S.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: cdk2]]
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[[Category: Cdk2]]
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[[Category: cell cycle]]
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[[Category: Cell cycle]]
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[[Category: mitosis]]
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[[Category: Mitosis]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: pyrazolopyrimidine inhibitor]]
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[[Category: Pyrazolopyrimidine inhibitor]]
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[[Category: serine/threonine protein kinase]]
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[[Category: Serine/threonine protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:01:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:00:19 2008''
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Revision as of 13:01, 3 May 2008

Image:1y91.gif

Template:STRUCTURE 1y91

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 Sat May 3 16:01:26 2008

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OCA

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