2h8h

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[[Image:2h8h.gif|left|200px]]
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{{Seed}}
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[[Image:2h8h.png|left|200px]]
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{{STRUCTURE_2h8h| PDB=2h8h | SCENE= }}
{{STRUCTURE_2h8h| PDB=2h8h | SCENE= }}
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'''Src kinase in complex with a quinazoline inhibitor'''
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===Src kinase in complex with a quinazoline inhibitor===
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==Overview==
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Src family kinases (SFKs) are nonreceptor tyrosine kinases that are reported to be critical for cancer progression. We report here a novel subseries of C-5-substituted anilinoquinazolines that display high affinity and specificity for the tyrosine kinase domain of the c-Src and Abl enzymes. These compounds exhibit high selectivity for SFKs over a panel of recombinant protein kinases, excellent pharmacokinetics, and in vivo activity following oral dosing. N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-( tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine (AZD0530) inhibits c-Src and Abl enzymes at low nanomolar concentrations and is highly selective over a range of kinases. AZD0530 displays excellent pharmacokinetic parameters in animal preclinically and in man (t(1/2) = 40 h). AZD0530 is a potent inhibitor of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo and led to a significant increase in survival in a highly aggressive, orthotopic model of human pancreatic cancer when dosed orally once daily. AZD0530 is currently undergoing clinical evaluation in man.
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The line below this paragraph, {{ABSTRACT_PUBMED_17064066}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17064066 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17064066}}
==About this Structure==
==About this Structure==
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[[Category: Rowsell, S.]]
[[Category: Rowsell, S.]]
[[Category: Src kinase]]
[[Category: Src kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:59:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 17:15:19 2008''

Revision as of 14:15, 28 July 2008

Image:2h8h.png

Template:STRUCTURE 2h8h

Src kinase in complex with a quinazoline inhibitor

Template:ABSTRACT PUBMED 17064066

About this Structure

2H8H is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor., Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A, Otterbein L, Ple PA, Warin N, Costello G, J Med Chem. 2006 Nov 2;49(22):6465-88. PMID:17064066

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