1e8x: Difference between revisions

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[[Image:1e8x.gif|left|200px]]
{{Seed}}
[[Image:1e8x.png|left|200px]]


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{{STRUCTURE_1e8x|  PDB=1e8x  |  SCENE=  }}  
{{STRUCTURE_1e8x|  PDB=1e8x  |  SCENE=  }}  


'''STRUCTURAL INSIGHTS INTO PHOSHOINOSITIDE 3-KINASE ENZYMATIC MECHANISM AND SIGNALLING'''
===STRUCTURAL INSIGHTS INTO PHOSHOINOSITIDE 3-KINASE ENZYMATIC MECHANISM AND SIGNALLING===




==Overview==
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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 degrees rotations. Staurosporine/PI3K interactions are reminiscent of low-affinity protein kinase/staurosporine complexes. These results provide a rich basis for development of isoform-specific PI3K inhibitors with therapeutic potential.
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{{ABSTRACT_PUBMED_11090628}}


==About this Structure==
==About this Structure==
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[[Category: Pi3k]]
[[Category: Pi3k]]
[[Category: Secondary messenger generation]]
[[Category: Secondary messenger generation]]
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Revision as of 21:20, 30 June 2008

File:1e8x.png

Template:STRUCTURE 1e8x

STRUCTURAL INSIGHTS INTO PHOSHOINOSITIDE 3-KINASE ENZYMATIC MECHANISM AND SIGNALLING

Template:ABSTRACT PUBMED 11090628

About this Structure

1E8X is a Single protein structure of sequence from Sus scrofa. This structure supersedes the now removed PDB entry 1qmm. 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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