2oh4

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[[Image:2oh4.jpg|left|200px]]
[[Image:2oh4.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2oh4 |SIZE=350|CAPTION= <scene name='initialview01'>2oh4</scene>, resolution 2.050&Aring;
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The line below this paragraph, containing "STRUCTURE_2oh4", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=GIG:METHYL+(5-{4-[({[2-FLUORO-5-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-1H-BENZIMIDAZOL-2-YL)CARBAMATE'>GIG</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= KDR, FLK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2oh4| PDB=2oh4 | SCENE= }}
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|RELATEDENTRY=[[1vr2|1vr2]], [[1y6a|1y6a]], [[1y6b|1y6b]], [[1ywm|1ywm]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2oh4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oh4 OCA], [http://www.ebi.ac.uk/pdbsum/2oh4 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oh4 RCSB]</span>
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}}
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'''Crystal structure of Vegfr2 with a benzimidazole-urea inhibitor'''
'''Crystal structure of Vegfr2 with a benzimidazole-urea inhibitor'''
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[[Category: Nolte, R T.]]
[[Category: Nolte, R T.]]
[[Category: Wang, L.]]
[[Category: Wang, L.]]
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[[Category: transferase]]
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[[Category: Transferase]]
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[[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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[[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 Mon Mar 31 04:17:50 2008''
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Revision as of 07:54, 4 May 2008

Image:2oh4.jpg

Template:STRUCTURE 2oh4

Crystal structure of Vegfr2 with a benzimidazole-urea inhibitor


Overview

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.

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 Page seeded by OCA on Sun May 4 10:54:20 2008

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OCA

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