2oo8: Difference between revisions

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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.
 
==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.F.]]
[[Category: Bellon, S F.]]
[[Category: Kim, J.]]
[[Category: Kim, J.]]
[[Category: RAJ]]
[[Category: RAJ]]
[[Category: kinase]]
[[Category: kinase]]


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