2qi8

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{{STRUCTURE_2qi8| PDB=2qi8 | SCENE= }}
{{STRUCTURE_2qi8| PDB=2qi8 | SCENE= }}
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'''Crystal structure of drug resistant SRC kinase domain'''
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===Crystal structure of drug resistant SRC kinase domain===
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==Overview==
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Resistance to kinase- targeted cancer drugs has recently been linked to a single point mutation in the ATP binding site of the kinase. In EGFR, the crucial Thr790 gatekeeper residue is mutated to a Met and prevents reversible ATP competitive inhibitors from binding. Irreversible 4-(phenylamino)quinazolines have been shown to overcome this drug resistance and are currently in clinical trials. In order to obtain a detailed structural understanding of how irreversible inhibitors overcome drug resistance, we used Src kinase as a model system for drug resistant EGFR-T790M. We report the first crystal structure of a drug resistant kinase in complex with an irreversible inhibitor. This 4-(phenylamino)quinazoline inhibits wild type and drug resistant EGFR in vitro at low nM concentrations. The co-crystal structure of drug resistant cSrc-T338M kinase domain provides the structural basis of this activity.
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(as it appears on PubMed at http://www.pubmed.gov), where 18316192 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18316192}}
==About this Structure==
==About this Structure==
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[[Category: Src kinase domain]]
[[Category: Src kinase domain]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 15:00:31 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 23 10:11:05 2008''

Revision as of 07:11, 23 July 2008

Image:2qi8.png

Template:STRUCTURE 2qi8

Crystal structure of drug resistant SRC kinase domain

Template:ABSTRACT PUBMED 18316192

About this Structure

2QI8 is a Single protein structure of sequence from Gallus gallus. Full crystallographic information is available from OCA.

Reference

Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR., Michalczyk A, Kluter S, Rode HB, Simard JR, Grutter C, Rabiller M, Rauh D, Bioorg Med Chem. 2008 Feb 20;. PMID:18316192

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