1oky

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(New page: 200px<br /> <applet load="1oky" size="450" color="white" frame="true" align="right" spinBox="true" caption="1oky, resolution 2.30&Aring;" /> '''STRUCTURE OF HUMAN ...)
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==About this Structure==
==About this Structure==
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1OKY 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 SO4, STU and GOL 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=1OKY OCA]].
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1OKY 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 SO4, STU and GOL 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: AC9. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1OKY 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: Aalten, D.M.F.Van.]]
[[Category: Aalten, D.M.F.Van.]]
[[Category: Alessi, D.R.]]
[[Category: Alessi, D.R.]]
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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 18:26:13 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 11:49:35 2007''

Revision as of 09:44, 30 October 2007


1oky, resolution 2.30Å

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STRUCTURE OF HUMAN PDK1 KINASE DOMAIN IN COMPLEX WITH STAUROSPORINE

Overview

PDK1 (3-phosphoinositide-dependent protein kinase-1) is a member of the, AGC (cAMP-dependent, cGMP-dependent, protein kinase C) family of protein, kinases, and has a key role in insulin and growth-factor signalling, through phosphorylation and subsequent activation of a number of other AGC, kinase family members, such as protein kinase B. The staurosporine, derivative UCN-01 (7-hydroxystaurosporine) has been reported to be a, potent inhibitor for PDK1, and is currently undergoing clinical trials for, the treatment of cancer. Here, we report the crystal structures of, staurosporine and UCN-01 in complex with the kinase domain of PDK1. We, show that, although staurosporine and UCN-01 interact with the PDK1 active, site in an overall similar manner, the UCN-01 7-hydroxy group, which is, not ... [(full description)]

About this Structure

1OKY is a [Single protein] structure of sequence from [Homo sapiens] with SO4, STU and GOL as [ligands]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: AC9. Full crystallographic information is available from [OCA].

Reference

Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition., Komander D, Kular GS, Bain J, Elliott M, Alessi DR, Van Aalten DM, Biochem J. 2003 Oct 15;375(Pt 2):255-62. PMID:12892559

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