1ckp

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[[Image:1ckp.gif|left|200px]]
[[Image:1ckp.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1ckp |SIZE=350|CAPTION= <scene name='initialview01'>1ckp</scene>, resolution 2.05&Aring;
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The line below this paragraph, containing "STRUCTURE_1ckp", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PVB:PURVALANOL'>PVB</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=
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|DOMAIN=
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{{STRUCTURE_1ckp| PDB=1ckp | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ckp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ckp OCA], [http://www.ebi.ac.uk/pdbsum/1ckp PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ckp RCSB]</span>
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}}
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'''HUMAN CYCLIN DEPENDENT KINASE 2 COMPLEXED WITH THE INHIBITOR PURVALANOL B'''
'''HUMAN CYCLIN DEPENDENT KINASE 2 COMPLEXED WITH THE INHIBITOR PURVALANOL B'''
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[[Category: Schultz, P G.]]
[[Category: Schultz, P G.]]
[[Category: Thunnissen, A M.W H.]]
[[Category: Thunnissen, A M.W H.]]
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[[Category: cell cycle]]
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[[Category: Cell cycle]]
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[[Category: cell division]]
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[[Category: Cell division]]
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[[Category: inhibition]]
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[[Category: Inhibition]]
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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: protein kinase]]
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[[Category: Protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 12:50:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 19:23:28 2008''
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Revision as of 09:50, 2 May 2008

Image:1ckp.gif

Template:STRUCTURE 1ckp

HUMAN CYCLIN DEPENDENT KINASE 2 COMPLEXED WITH THE INHIBITOR PURVALANOL B


Overview

Selective protein kinase inhibitors were developed on the basis of the unexpected binding mode of 2,6,9-trisubstituted purines to the adenosine triphosphate-binding site of the human cyclin-dependent kinase 2 (CDK2). By iterating chemical library synthesis and biological screening, potent inhibitors of the human CDK2-cyclin A kinase complex and of Saccharomyces cerevisiae Cdc28p were identified. The structural basis for the binding affinity and selectivity was determined by analysis of a three-dimensional crystal structure of a CDK2-inhibitor complex. The cellular effects of these compounds were characterized in mammalian cells and yeast. In the latter case the effects were characterized on a genome-wide scale by monitoring changes in messenger RNA levels in treated cells with high-density oligonucleotide probe arrays. Purine libraries could provide useful tools for analyzing a variety of signaling and regulatory pathways and may lead to the development of new therapeutics.

About this Structure

1CKP is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors., Gray NS, Wodicka L, Thunnissen AM, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L, Kim SH, Lockhart DJ, Schultz PG, Science. 1998 Jul 24;281(5376):533-8. PMID:9677190 Page seeded by OCA on Fri May 2 12:50:24 2008

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OCA

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