1v1k

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(New page: 200px<br /> <applet load="1v1k" size="450" color="white" frame="true" align="right" spinBox="true" caption="1v1k, resolution 2.31&Aring;" /> '''CDK2 IN COMPLEX WIT...)
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==About this Structure==
==About this Structure==
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1V1K is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with ACE and 3FP as [[http://en.wikipedia.org/wiki/ligands ligands]]. This structure superseeds the now removed PDB entry 1H06. 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=1V1K OCA]].
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1V1K is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with ACE and 3FP as [[http://en.wikipedia.org/wiki/ligands ligands]]. This structure superseeds the now removed PDB entry 1H06. 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=1V1K OCA]].
==Reference==
==Reference==
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Transferred entry: 2.7.11.1]]
[[Category: Beattie, J.F.]]
[[Category: Beattie, J.F.]]
[[Category: Breault, G.A.]]
[[Category: Breault, G.A.]]
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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 19:30:21 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 12:37:15 2007''

Revision as of 10:32, 30 October 2007


1v1k, resolution 2.31Å

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CDK2 IN COMPLEX WITH A DISUBSTITUTED 4, 6-BIS ANILINO PYRIMIDINE CDK4 INHIBITOR

Overview

Using a high-throughput screening campaign, we identified the 4,6-bis, anilino pyrimidines as inhibitors of the cyclin-dependent kinase, CDK4., Herein we describe the further chemical modification and use of X-ray, crystallography to develop potent and selective in vitro inhibitors of, CDK4.

About this Structure

1V1K is a [Single protein] structure of sequence from [Homo sapiens] with ACE and 3FP as [ligands]. This structure superseeds the now removed PDB entry 1H06. 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

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines., Beattie JF, Breault GA, Ellston RP, Green S, Jewsbury PJ, Midgley CJ, Naven RT, Minshull CA, Pauptit RA, Tucker JA, Pease JE, Bioorg Med Chem Lett. 2003 Sep 15;13(18):2955-60. PMID:12941311

Page seeded by OCA on Tue Oct 30 12:37:15 2007

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