2osc: Difference between revisions

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==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==

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[[Category: Receptor protein-tyrosine kinase]]

[[Category: Single protein]]

[[Category: Bellon, S.F.]]

[[Category: Bellon, S F.]]

[[Category: Kim, J.]]

[[Category: MUH]]

[[Category: kinase domain tie-2]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:21:59 2008''

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@@ Line 4: / Line 4: @@
 ==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==
@@ Line 14: / Line 17: @@
 [[Category: Receptor protein-tyrosine kinase]]
 [[Category: Single protein]]
-[[Category: Bellon, S.F.]]
+[[Category: Bellon, S F.]]
 [[Category: Kim, J.]]
 [[Category: MUH]]
 [[Category: kinase domain tie-2]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 15:04:33 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:21:59 2008''