2b52

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(New page: 200px<br /> <applet load="2b52" size="450" color="white" frame="true" align="right" spinBox="true" caption="2b52, resolution 1.88&Aring;" /> '''Human cyclin depend...)
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Revision as of 18:52, 12 November 2007

Image:2b52.gif

2b52, resolution 1.88Å

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Human cyclin dependent kinase 2 (CDK2) complexed with DPH-042562

Overview

New indeno[1,2-c]pyrazol-4-one cyclin dependent kinase inhibitors have, been disclosed. The most promising compounds are nanomolar enzyme, inhibitors with excellent activity against tumor cells. The most advanced, compound retains cell culture activity even in the presence of human serum, proteins. The most advanced compound did not kill the normal fibroblast, line AG1523.

About this Structure

2B52 is a Single protein structure of sequence from Homo sapiens with D42 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

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3., Yue EW, DiMeo SV, Higley CA, Markwalder JA, Burton CR, Benfield PA, Grafstrom RH, Cox S, Muckelbauer JK, Smallwood AM, Chen H, Chang CH, Trainor GL, Seitz SP, Bioorg Med Chem Lett. 2004 Jan 19;14(2):343-6. PMID:14698155

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