2e2b

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[[Image:2e2b.jpg|left|200px]]
[[Image:2e2b.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2e2b |SIZE=350|CAPTION= <scene name='initialview01'>2e2b</scene>, resolution 2.2&Aring;
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The line below this paragraph, containing "STRUCTURE_2e2b", 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=406:N-[3-(4,5&#39;-BIPYRIMIDIN-2-YLAMINO)-4-METHYLPHENYL]-4-{[(3S)-3-(DIMETHYLAMINO)PYRROLIDIN-1-YL]METHYL}-3-(TRIFLUOROMETHYL)BENZAMIDE'>406</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/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_2e2b| PDB=2e2b | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2e2b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2e2b OCA], [http://www.ebi.ac.uk/pdbsum/2e2b PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2e2b RCSB]</span>
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}}
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'''Crystal structure of the c-Abl kinase domain in complex with INNO-406'''
'''Crystal structure of the c-Abl kinase domain in complex with INNO-406'''
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[[Category: Takagaki, K.]]
[[Category: Takagaki, K.]]
[[Category: Wakayama, T.]]
[[Category: Wakayama, T.]]
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[[Category: c-abl]]
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[[Category: C-abl]]
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[[Category: inno-406]]
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[[Category: Inno-406]]
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[[Category: kinase]]
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[[Category: Kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 01:47:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:42:38 2008''
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Revision as of 22:47, 3 May 2008

Image:2e2b.jpg

Template:STRUCTURE 2e2b

Crystal structure of the c-Abl kinase domain in complex with INNO-406


Overview

To investigate why 3-substituted benzamide derivatives show dual inhibition of Abl and Lyn protein tyrosine kinases, we determined their inhibitory activities against Abl and Lyn, carried out molecular modeling, and conducted a structure-activity relationship study with the aid of a newly determined X-ray structure of the Abl/Lyn dual inhibitor INNO-406 (formerly known as NS-187) bound to human Abl. We found that this series of compounds interacted with both kinases in very similar ways, so that they can inhibit both kinases effectively.

About this Structure

2E2B is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives., Horio T, Hamasaki T, Inoue T, Wakayama T, Itou S, Naito H, Asaki T, Hayase H, Niwa T, Bioorg Med Chem Lett. 2007 May 15;17(10):2712-7. Epub 2007 Mar 3. PMID:17376680 Page seeded by OCA on Sun May 4 01:47:30 2008

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