2oh4: Difference between revisions

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[[Image:2oh4.jpg|left|200px]]
{{Seed}}
[[Image:2oh4.png|left|200px]]


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{{STRUCTURE_2oh4|  PDB=2oh4  |  SCENE=  }}  
{{STRUCTURE_2oh4|  PDB=2oh4  |  SCENE=  }}  


'''Crystal structure of Vegfr2 with a benzimidazole-urea inhibitor'''
===Crystal structure of Vegfr2 with a benzimidazole-urea inhibitor===




==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.
The line below this paragraph, {{ABSTRACT_PUBMED_17676829}}, adds the Publication Abstract to the page
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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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