2oj9: Difference between revisions
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New page: left|200px<br /> <applet load="2oj9" size="450" color="white" frame="true" align="right" spinBox="true" caption="2oj9, resolution 2.00Å" /> '''Structure of IGF-1R... |
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[[Image:2oj9.gif|left|200px]]<br /> | [[Image:2oj9.gif|left|200px]]<br /><applet load="2oj9" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2oj9" size=" | |||
caption="2oj9, resolution 2.00Å" /> | caption="2oj9, resolution 2.00Å" /> | ||
'''Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor'''<br /> | '''Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor'''<br /> | ||
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==Overview== | ==Overview== | ||
The discovery and synthesis of, 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like, growth factor 1-receptor (IGF-1R) are presented. Installing amine, containing side chains at the 4-position of pyridone ring significantly, improved the enzyme potency. SAR and biological activity of these, compounds is presented. | The discovery and synthesis of, 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like, growth factor 1-receptor (IGF-1R) are presented. Installing amine, containing side chains at the 4-position of pyridone ring significantly, improved the enzyme potency. SAR and biological activity of these, compounds is presented. | ||
==About this Structure== | ==About this Structure== | ||
2OJ9 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 BMI as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] Full crystallographic information is available from [http:// | 2OJ9 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=BMI:'>BMI</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OJ9 OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: kinase domain]] | [[Category: kinase domain]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 15:28:23 2008'' | ||
