1uvr
From Proteopedia
(New page: 200px<br /> <applet load="1uvr" size="450" color="white" frame="true" align="right" spinBox="true" caption="1uvr, resolution 2.81Å" /> '''STRUCTURE OF HUMAN ...) |
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==About this Structure== | ==About this Structure== | ||
| - | 1UVR 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, BI8 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=1UVR OCA]]. | + | 1UVR 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, BI8 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: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1UVR OCA]]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| + | [[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]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 13:10:48 2007'' |
Revision as of 11:06, 30 October 2007
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STRUCTURE OF HUMAN PDK1 KINASE DOMAIN IN COMPLEX WITH BIM-8
Overview
LY333531, BIM-1, BIM-2, BIM-3, and BIM-8 are bisindolyl maleimide-based, nanomolar protein kinase C inhibitors. LY333531, a PKCbeta-specific, inhibitor, is in clinical trials against diabetes and cardiac ventricular, hypertrophy complications. Specificity analysis with a panel of 29 protein, kinases reveals that these bisindolyl maleimide inhibitors also inhibit, PDK1, a key kinase from the insulin signaling pathway, albeit in the lower, microM range. To understand the molecular basis of inhibition, the PDK1, kinase domain was cocrystallized with these bisindolyl maleimide, inhibitors. The inhibitor complexes represent the first structural, description of this class of compounds, revealing their unusual nonplanar, conformation within the ATP binding site and also explaining the higher, ... [(full description)]
About this Structure
1UVR is a [Single protein] structure of sequence from [Homo sapiens] with SO4, BI8 and GOL 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
Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1., Komander D, Kular GS, Schuttelkopf AW, Deak M, Prakash KR, Bain J, Elliott M, Garrido-Franco M, Kozikowski AP, Alessi DR, van Aalten DM, Structure. 2004 Feb;12(2):215-26. PMID:14962382
Page seeded by OCA on Tue Oct 30 13:10:48 2007
Categories: Homo sapiens | Single protein | Transferred entry: 2.7.11.1 | Aalten, D.M.F.Van. | Alessi, D.R. | Bain, J. | Deak, M. | Elliot, M. | Garrido-Franco, M. | Komander, D. | Kozikowski, A.P. | Kular, G.S. | Prakash, K.R. | Schuttelkopf, A.W. | BI8 | GOL | SO4 | Bim-8 | Bisindolyl maleimide | Cancer | Diabetes | Inhibitor | Ly333531 | Pdk1 | Pkb | Protein kinase | Transferase
