2oo8: Difference between revisions
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==Overview== | ==Overview== | ||
A novel class of selective Tie-2 inhibitors was derived from a | 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. | ||
==Disease== | |||
Known diseases associated with this structure: Venous malformations, multiple cutaneous and mucosal OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=600221 600221]] | |||
==About this Structure== | ==About this Structure== | ||
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[[Category: Receptor protein-tyrosine kinase]] | [[Category: Receptor protein-tyrosine kinase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Bellon, S | [[Category: Bellon, S F.]] | ||
[[Category: Kim, J.]] | [[Category: Kim, J.]] | ||
[[Category: RAJ]] | [[Category: RAJ]] | ||
[[Category: kinase]] | [[Category: kinase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:20:50 2008'' |