2b53

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(New page: 200px<br /> <applet load="2b53" size="450" color="white" frame="true" align="right" spinBox="true" caption="2b53, resolution 2.00&Aring;" /> '''Human cyclin depend...)
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Revision as of 18:52, 12 November 2007

Image:2b53.gif

2b53, resolution 2.00Å

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Human cyclin dependent kinase 2 (CDK2) complexed with DIN-234325

Overview

Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E., Aspects of the SAR were investigated using solution-phase, parallel, synthesis. An X-ray crystal structure was obtained of quinazoline 51 bound, in CDK2 and key interactions within the ATP binding pocket are defined.

About this Structure

2B53 is a Single protein structure of sequence from Homo sapiens with D23 as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.

Reference

Quinazolines as cyclin dependent kinase inhibitors., Sielecki TM, Johnson TL, Liu J, Muckelbauer JK, Grafstrom RH, Cox S, Boylan J, Burton CR, Chen H, Smallwood A, Chang CH, Boisclair M, Benfield PA, Trainor GL, Seitz SP, Bioorg Med Chem Lett. 2001 May 7;11(9):1157-60. PMID:11354366

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