2iw9

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:2iw9.gif|left|200px]]
[[Image:2iw9.gif|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 2iw9 |SIZE=350|CAPTION= <scene name='initialview01'>2iw9</scene>, resolution 2.00&Aring;
+
The line below this paragraph, containing "STRUCTURE_2iw9", creates the "Structure Box" on the page.
-
|SITE= <scene name='pdbsite=AC1:4sp+Binding+Site+For+Chain+C'>AC1</scene>
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=4SP:O6-CYCLOHEXYLMETHOXY-2-(4&#39;-SULPHAMOYLANILINO)+PURINE'>4SP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=SGM:MONOTHIOGLYCEROL'>SGM</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|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>
+
or leave the SCENE parameter empty for the default display.
-
|GENE=
+
-->
-
|DOMAIN=
+
{{STRUCTURE_2iw9| PDB=2iw9 | SCENE= }}
-
|RELATEDENTRY=
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2iw9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2iw9 OCA], [http://www.ebi.ac.uk/pdbsum/2iw9 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2iw9 RCSB]</span>
+
-
}}
+
'''STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A COMPLEXED WITH A BISANILINOPYRIMIDINE INHIBITOR'''
'''STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A COMPLEXED WITH A BISANILINOPYRIMIDINE INHIBITOR'''
Line 32: Line 29:
[[Category: Noble, M E.M.]]
[[Category: Noble, M E.M.]]
[[Category: Pratt, D J.]]
[[Category: Pratt, D J.]]
-
[[Category: atp-binding]]
+
[[Category: Atp-binding]]
-
[[Category: cell cycle]]
+
[[Category: Cell cycle]]
-
[[Category: cell cycle complex]]
+
[[Category: Cell cycle complex]]
-
[[Category: cell division]]
+
[[Category: Cell division]]
-
[[Category: cyclin]]
+
[[Category: Cyclin]]
-
[[Category: kinase]]
+
[[Category: Kinase]]
-
[[Category: mitosis]]
+
[[Category: Mitosis]]
-
[[Category: nucleotide-binding]]
+
[[Category: Nucleotide-binding]]
-
[[Category: phosphorylation]]
+
[[Category: Phosphorylation]]
-
[[Category: polymorphism]]
+
[[Category: Polymorphism]]
-
[[Category: serine-threonine-protein kinase]]
+
[[Category: Serine-threonine-protein kinase]]
-
[[Category: serine/threonine-protein kinase]]
+
[[Category: Serine/threonine-protein kinase]]
-
[[Category: transferase]]
+
[[Category: Transferase]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:58:27 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:49:30 2008''
+

Revision as of 04:58, 4 May 2008

Image:2iw9.gif

Template:STRUCTURE 2iw9

STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A COMPLEXED WITH A BISANILINOPYRIMIDINE 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

2IW9 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 07:58:27 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2iw9"
Personal tools