1y91

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[[Image:1y91.gif|left|200px]]<br /><applet load="1y91" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1y91.gif|left|200px]]
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caption="1y91, resolution 2.15&Aring;" />
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'''Crystal structure of human CDK2 complexed with a pyrazolo[1,5-a]pyrimidine inhibitor'''<br />
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{{Structure
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|PDB= 1y91 |SIZE=350|CAPTION= <scene name='initialview01'>1y91</scene>, resolution 2.15&Aring;
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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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|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]
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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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}}
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'''Crystal structure of human CDK2 complexed with a pyrazolo[1,5-a]pyrimidine inhibitor'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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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].
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1Y91 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Y91 OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15686876 15686876]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/15686876 15686876]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: serine/threonine protein kinase]]
[[Category: serine/threonine protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:02:56 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:19:53 2008''

Revision as of 13:19, 20 March 2008

Image:1y91.gif


PDB ID 1y91

Drag the structure with the mouse to rotate
, resolution 2.15Å
Ligands:
Gene: CDK2 (Homo sapiens)
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
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 Thu Mar 20 15:19:53 2008

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