View source for 2iw6

[[Image:2iw6.gif|left|200px]]<br />
<applet load="2iw6" size="450" color="white" frame="true" align="right" spinBox="true" 
caption="2iw6, resolution 2.30&Aring;" />
'''STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A COMPLEXED WITH A BISANILINOPYRIMIDINE INHIBITOR'''<br />

==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. ... [[http://ispc.weizmann.ac.il/pmbin/getpm?16942020 (full description)]]

==About this Structure==
2IW6 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 MG, QQ2 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=2IW6 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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16942020 16942020]
[[Category: Homo sapiens]]
[[Category: Protein complex]]
[[Category: Bentley, J.]]
[[Category: Boyle, F.T.]]
[[Category: Endicott, J.A.]]
[[Category: Jewsbury, P.]]
[[Category: Noble, M.E.M.]]
[[Category: Pratt, D.J.]]
[[Category: MG]]
[[Category: QQ2]]
[[Category: SGM]]
[[Category: atp-binding]]
[[Category: cell cycle]]
[[Category: cell cycle complex]]
[[Category: cell division]]
[[Category: cyclin]]
[[Category: kinase]]
[[Category: mitosis]]
[[Category: nucleotide-binding]]
[[Category: phosphorylation]]
[[Category: polymorphism]]
[[Category: serine-threonine-protein kinase]]
[[Category: serine/threonine-protein kinase]]
[[Category: transferase]]

''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Oct 29 18:11:57 2007''