2bkz

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(New page: 200px<br /> <applet load="2bkz" size="450" color="white" frame="true" align="right" spinBox="true" caption="2bkz, resolution 2.60&Aring;" /> '''STRUCTURE OF CDK2-C...)
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==About this Structure==
==About this Structure==
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2BKZ 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 SO4 and SBC 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=2BKZ OCA]].
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2BKZ 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 SO4 and SBC 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=2BKZ 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: Bargiottia, A.]]
[[Category: Bargiottia, A.]]
[[Category: Brasca, M.G.]]
[[Category: Brasca, M.G.]]
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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 21:34:25 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 14:07:21 2007''

Revision as of 12:02, 30 October 2007


2bkz, resolution 2.60Å

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STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611

Overview

The synthesis and the preliminary expansion of this new class of CDK2, inhibitors are presented. The synthesis was accomplished using a, solution-phase protocol amenable to rapid parallel expansion and suitable, to be scaled-up in view of possible lead development. Following a, medicinal chemistry program aimed at improving cell permeability and, selectivity, a series of compounds with nanomolar activity in the, biochemical assay and able to efficiently inhibit tumor cell proliferation, has been obtained.

About this Structure

2BKZ is a [Protein complex] structure of sequences from [Homo sapiens] with SO4 and SBC 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

Benzodipyrazoles: a new class of potent CDK2 inhibitors., D'Alessio R, Bargiotti A, Metz S, Brasca MG, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez ML, Vulpetti A, Pevarello P, Bioorg Med Chem Lett. 2005 Mar 1;15(5):1315-9. PMID:15713378

Page seeded by OCA on Tue Oct 30 14:07:21 2007

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