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2itt

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[[Image:2itt.jpg|left|200px]]
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{{Seed}}
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[[Image:2itt.png|left|200px]]
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{{STRUCTURE_2itt| PDB=2itt | SCENE= }}
{{STRUCTURE_2itt| PDB=2itt | SCENE= }}
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'''CRYSTAL STRUCTURE OF EGFR KINASE DOMAIN L858R MUTATION IN COMPLEX WITH AEE788'''
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===CRYSTAL STRUCTURE OF EGFR KINASE DOMAIN L858R MUTATION IN COMPLEX WITH AEE788===
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==Overview==
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Mutations in the EGFR kinase are a cause of non-small-cell lung cancer. To understand their mechanism of activation and effects on drug binding, we studied the kinetics of the L858R and G719S mutants and determined their crystal structures with inhibitors including gefitinib, AEE788, and a staurosporine. We find that the mutations activate the kinase by disrupting autoinhibitory interactions, and that they accelerate catalysis as much as 50-fold in vitro. Structures of inhibitors in complex with both wild-type and mutant kinases reveal similar binding modes for gefitinib and AEE788, but a marked rotation of the staurosporine in the G719S mutant. Strikingly, direct binding measurements show that gefitinib binds 20-fold more tightly to the L858R mutant than to the wild-type enzyme.
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The line below this paragraph, {{ABSTRACT_PUBMED_17349580}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17349580 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17349580}}
==About this Structure==
==About this Structure==
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[[Category: Transmembrane]]
[[Category: Transmembrane]]
[[Category: Tyrosine-protein kinase]]
[[Category: Tyrosine-protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:51:33 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:35:26 2008''

Revision as of 12:35, 28 July 2008

Image:2itt.png

Template:STRUCTURE 2itt

CRYSTAL STRUCTURE OF EGFR KINASE DOMAIN L858R MUTATION IN COMPLEX WITH AEE788

Template:ABSTRACT PUBMED 17349580

About this Structure

2ITT is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity., Yun CH, Boggon TJ, Li Y, Woo MS, Greulich H, Meyerson M, Eck MJ, Cancer Cell. 2007 Mar;11(3):217-27. PMID:17349580

Page seeded by OCA on Mon Jul 28 15:35:26 2008

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