2e2b: Difference between revisions
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New page: left|200px<br /> <applet load="2e2b" size="450" color="white" frame="true" align="right" spinBox="true" caption="2e2b, resolution 2.2Å" /> '''Crystal structure of... |
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[[Image:2e2b. | [[Image:2e2b.jpg|left|200px]]<br /><applet load="2e2b" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2e2b" size=" | |||
caption="2e2b, resolution 2.2Å" /> | caption="2e2b, resolution 2.2Å" /> | ||
'''Crystal structure of the c-Abl kinase domain in complex with INNO-406'''<br /> | '''Crystal structure of the c-Abl kinase domain in complex with INNO-406'''<br /> | ||
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==Overview== | ==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. | 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== | ==About this Structure== | ||
2E2B is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with 406 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http:// | 2E2B is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=406:'>406</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2E2B OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: kinase]] | [[Category: kinase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 15:10:49 2008'' | ||
