2iw8

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(New page: 200px<br /> <applet load="2iw8" size="450" color="white" frame="true" align="right" spinBox="true" caption="2iw8, resolution 2.30&Aring;" /> '''STRUCTURE OF HUMAN ...)
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==About this Structure==
==About this Structure==
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2IW8 is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with 4SP and SGM as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2IW8 OCA]].
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2IW8 is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with 4SP and SGM as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[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]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2IW8 OCA]].
==Reference==
==Reference==
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: Transferred entry: 2.7.11.1]]
[[Category: Bentley, J.]]
[[Category: Bentley, J.]]
[[Category: Boyle, F.T.]]
[[Category: Boyle, F.T.]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Oct 29 18:11:28 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 11:38:55 2007''

Revision as of 09:34, 30 October 2007


2iw8, resolution 2.30Å

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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. ... [(full description)]

About this Structure

2IW8 is a [Protein complex] structure of sequences from [Homo sapiens] with 4SP and SGM as [ligands]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: AC1. 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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