2oo8: Difference between revisions
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New page: left|200px<br /> <applet load="2oo8" size="450" color="white" frame="true" align="right" spinBox="true" caption="2oo8, resolution 2.20Å" /> '''Synthesis, Structur... |
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[[Image:2oo8.gif|left|200px]]<br /> | [[Image:2oo8.gif|left|200px]]<br /><applet load="2oo8" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2oo8" size=" | |||
caption="2oo8, resolution 2.20Å" /> | caption="2oo8, resolution 2.20Å" /> | ||
'''Synthesis, Structural Analysis, and SAR Studies of Triazine Derivatives as Potent, Selective Tie-2 Inhibitors'''<br /> | '''Synthesis, Structural Analysis, and SAR Studies of Triazine Derivatives as Potent, Selective Tie-2 Inhibitors'''<br /> | ||
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==Overview== | ==Overview== | ||
A novel class of selective Tie-2 inhibitors was derived from a, multi-kinase inhibitor 1. By reversing the amide connectivity and, incorporating aminotriazine or aminopyridine hinge-binding moieties, excellent Tie-2 potency and KDR selectivity could be achieved with, 3-substituted terminal aryl rings. X-ray co-crystal structure analysis, aided inhibitor design. This series was evaluated on the basis of potency, selectivity, and rat pharmacokinetic parameters. | A novel class of selective Tie-2 inhibitors was derived from a, multi-kinase inhibitor 1. By reversing the amide connectivity and, incorporating aminotriazine or aminopyridine hinge-binding moieties, excellent Tie-2 potency and KDR selectivity could be achieved with, 3-substituted terminal aryl rings. X-ray co-crystal structure analysis, aided inhibitor design. This series was evaluated on the basis of potency, selectivity, and rat pharmacokinetic parameters. | ||
==About this Structure== | ==About this Structure== | ||
2OO8 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 RAJ as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http:// | 2OO8 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=RAJ:'>RAJ</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OO8 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 15:04:24 2008'' | ||
