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2iw8

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[[Image:2iw8.gif|left|200px]]
[[Image:2iw8.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2iw8 |SIZE=350|CAPTION= <scene name='initialview01'>2iw8</scene>, resolution 2.30&Aring;
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The line below this paragraph, containing "STRUCTURE_2iw8", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:4sp+Binding+Site+For+Chain+C'>AC1</scene>
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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=4SP:O6-CYCLOHEXYLMETHOXY-2-(4&#39;-SULPHAMOYLANILINO)+PURINE'>4SP</scene>, <scene name='pdbligand=SGM:MONOTHIOGLYCEROL'>SGM</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</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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-->
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|DOMAIN=
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{{STRUCTURE_2iw8| PDB=2iw8 | 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=2iw8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2iw8 OCA], [http://www.ebi.ac.uk/pdbsum/2iw8 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2iw8 RCSB]</span>
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}}
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'''STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A F82H-L83V-H84D MUTANT WITH AN O6-CYCLOHEXYLMETHYLGUANINE INHIBITOR'''
'''STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A F82H-L83V-H84D MUTANT WITH AN O6-CYCLOHEXYLMETHYLGUANINE INHIBITOR'''
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[[Category: Noble, M E.M.]]
[[Category: Noble, M E.M.]]
[[Category: Pratt, D J.]]
[[Category: Pratt, D J.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: cell cycle]]
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[[Category: Cell cycle]]
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[[Category: cell cycle complex]]
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[[Category: Cell cycle complex]]
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[[Category: cell division]]
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[[Category: Cell division]]
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[[Category: cyclin]]
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[[Category: Cyclin]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: mitosis]]
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[[Category: Mitosis]]
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[[Category: nucleotide-binding]]
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[[Category: Nucleotide-binding]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: polymorphism]]
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[[Category: Polymorphism]]
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[[Category: serine-threonine-protein kinase]]
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[[Category: Serine-threonine-protein kinase]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:58:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:49:30 2008''
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Revision as of 04:58, 4 May 2008

Image:2iw8.gif

Template:STRUCTURE 2iw8

STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A F82H-L83V-H84D MUTANT WITH AN O6-CYCLOHEXYLMETHYLGUANINE INHIBITOR


Overview

Cyclin dependent kinases are a key family of kinases involved in cell cycle regulation and are an attractive target for cancer chemotherapy. The roles of four residues of the cyclin-dependent kinase active site in inhibitor selectivity were investigated by producing cyclin-dependent kinase 2 mutants bearing equivalent cyclin-dependent kinase 4 residues, namely F82H, L83V, H84D, and K89T. Assay of the mutants with a cyclin-dependent kinase 4-selective bisanilinopyrimidine shows that the K89T mutation is primarily responsible for the selectivity of this compound. Use of the cyclin-dependent kinase 2-selective 6-cyclohexylmethoxy-2-(4'-sulfamoylanilino)purine (NU6102) shows that K89T has no role in the selectivity, while the remaining three mutations have a cumulative influence. The results indicate that certain residues that are not frequently considered in structure-aided kinase inhibitor design have an important role to play.

About this Structure

2IW8 is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity., Pratt DJ, Bentley J, Jewsbury P, Boyle FT, Endicott JA, Noble ME, J Med Chem. 2006 Sep 7;49(18):5470-7. PMID:16942020 Page seeded by OCA on Sun May 4 07:58:23 2008

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