2iw8

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|PDB= 2iw8 |SIZE=350|CAPTION= <scene name='initialview01'>2iw8</scene>, resolution 2.30&Aring;
|PDB= 2iw8 |SIZE=350|CAPTION= <scene name='initialview01'>2iw8</scene>, resolution 2.30&Aring;
|SITE= <scene name='pdbsite=AC1:4sp+Binding+Site+For+Chain+C'>AC1</scene>
|SITE= <scene name='pdbsite=AC1:4sp+Binding+Site+For+Chain+C'>AC1</scene>
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|LIGAND= <scene name='pdbligand=4SP:O6-CYCLOHEXYLMETHOXY-2-(4'-SULPHAMOYLANILINO)+PURINE'>4SP</scene> and <scene name='pdbligand=SGM:MONOTHIOGLYCEROL'>SGM</scene>
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|LIGAND= <scene name='pdbligand=4SP:O6-CYCLOHEXYLMETHOXY-2-(4&#39;-SULPHAMOYLANILINO)+PURINE'>4SP</scene> and <scene name='pdbligand=SGM:MONOTHIOGLYCEROL'>SGM</scene>
|ACTIVITY= [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]
|ACTIVITY= [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]
|GENE=
|GENE=
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:34:08 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 23 15:22:51 2008''

Revision as of 13:22, 23 March 2008

Image:2iw8.gif


PDB ID 2iw8

Drag the structure with the mouse to rotate
, resolution 2.30Å
Sites:
Ligands: and
Activity: Transferred entry: 2.7.11.1, with EC number 2.7.1.37
Coordinates: save as pdb, mmCIF, xml



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

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