2oh4

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{{STRUCTURE_2oh4| PDB=2oh4 | SCENE= }}
{{STRUCTURE_2oh4| PDB=2oh4 | SCENE= }}
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'''Crystal structure of Vegfr2 with a benzimidazole-urea inhibitor'''
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===Crystal structure of Vegfr2 with a benzimidazole-urea inhibitor===
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==Overview==
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We herein disclose a novel chemical series of benzimidazole-ureas as inhibitors of VEGFR-2 and TIE-2 kinase receptors, both of which are implicated in angiogenesis. Structure-activity relationship (SAR) studies elucidated a critical role for the N1 nitrogen of both the benzimidazole (segment E) and urea (segment B) moieties. The SAR results were also supported by the X-ray crystallographic elucidation of the role of the N1 nitrogen and the urea moiety when the benzimidazole-urea compounds were bound to the VEGFR-2 enzyme. The left side phenyl ring (segment A) occupies the backpocket where a 3-hydrophobic substituent was favored for TIE-2 activity.
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{{ABSTRACT_PUBMED_17676829}}
==About this Structure==
==About this Structure==
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[[Category: Transferase]]
[[Category: Transferase]]
[[Category: Vascular endothelial growth factor receptor 2 tyrosine-protein kinase 3d-structure vegfr2 angiogenesis atp-binding phosphorylation ec 2 7.1 112 vegfr-2 kinase insert domain receptor protein-tyrosine kinase receptor flk-1]]
[[Category: Vascular endothelial growth factor receptor 2 tyrosine-protein kinase 3d-structure vegfr2 angiogenesis atp-binding phosphorylation ec 2 7.1 112 vegfr-2 kinase insert domain receptor protein-tyrosine kinase receptor flk-1]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:54:20 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 12:53:14 2008''

Revision as of 09:53, 27 July 2008

Image:2oh4.png

Template:STRUCTURE 2oh4

Crystal structure of Vegfr2 with a benzimidazole-urea inhibitor

Template:ABSTRACT PUBMED 17676829

About this Structure

2OH4 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery of novel benzimidazoles as potent inhibitors of TIE-2 and VEGFR-2 tyrosine kinase receptors., Hasegawa M, Nishigaki N, Washio Y, Kano K, Harris PA, Sato H, Mori I, West RI, Shibahara M, Toyoda H, Wang L, Nolte RT, Veal JM, Cheung M, J Med Chem. 2007 Sep 6;50(18):4453-70. Epub 2007 Aug 4. PMID:17676829

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