1e7v
From Proteopedia
(New page: 200px<br /> <applet load="1e7v" size="450" color="white" frame="true" align="right" spinBox="true" caption="1e7v, resolution 2.40Å" /> '''STRUCTURE DETERMINA...) |
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==About this Structure== | ==About this Structure== | ||
| - | 1E7V is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Sus_scrofa Sus scrofa]] with LY2 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.137 2.7.1.137]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1E7V OCA]]. | + | 1E7V is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Sus_scrofa Sus scrofa]] with LY2 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/Phosphatidylinositol_3-kinase Phosphatidylinositol 3-kinase]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.137 2.7.1.137]]. Structure known Active Site: LY2. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1E7V OCA]]. |
==Reference== | ==Reference== | ||
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine., Walker EH, Pacold ME, Perisic O, Stephens L, Hawkins PT, Wymann MP, Williams RL, Mol Cell. 2000 Oct;6(4):909-19. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11090628 11090628] | Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine., Walker EH, Pacold ME, Perisic O, Stephens L, Hawkins PT, Wymann MP, Williams RL, Mol Cell. 2000 Oct;6(4):909-19. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11090628 11090628] | ||
| + | [[Category: Phosphatidylinositol 3-kinase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Sus scrofa]] | [[Category: Sus scrofa]] | ||
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[[Category: secondary messenger generation]] | [[Category: secondary messenger generation]] | ||
| - | ''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 11:03:16 2007'' |
Revision as of 08:58, 30 October 2007
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STRUCTURE DETERMINANTS OF PHOSPHOINOSITIDE 3-KINASE INHIBITION BY WORTMANNIN, LY294002, QUERCETIN, MYRICETIN AND STAUROSPORINE
Overview
The specific phosphoinositide 3-kinase (PI3K) inhibitors wortmannin and, LY294002 have been invaluable tools for elucidating the roles of these, enzymes in signal transduction pathways. The X-ray crystallographic, structures of PI3Kgamma bound to these lipid kinase inhibitors and to the, broad-spectrum protein kinase inhibitors quercetin, myricetin, and, staurosporine reveal how these compounds fit into the ATP binding pocket., With a nanomolar IC50, wortmannin most closely fits and fills the active, site and induces a conformational change in the catalytic domain., Surprisingly, LY294002 and the lead compound on which it was designed, quercetin, as well as the closely related flavonoid myricetin bind PI3K in, remarkably different orientations that are related to each other by 180, ... [(full description)]
About this Structure
1E7V is a [Single protein] structure of sequence from [Sus scrofa] with LY2 as [ligand]. Active as [Phosphatidylinositol 3-kinase], with EC number [2.7.1.137]. Structure known Active Site: LY2. Full crystallographic information is available from [OCA].
Reference
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine., Walker EH, Pacold ME, Perisic O, Stephens L, Hawkins PT, Wymann MP, Williams RL, Mol Cell. 2000 Oct;6(4):909-19. PMID:11090628
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