2ea2: Difference between revisions

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==Overview==

A series of aryl sulfonamides of 5,6-disubstituted anthranilic acids were, identified as potent inhibitors of methionine aminopeptidase-2 (MetAP2)., Small alkyl groups and 3-furyl were tolerated at the 5-position of, anthranilic acid, while -OCH(3), CH(3), and Cl were found optimal for the, 6-position. Placement of 2-aminoethoxy group at the 6-position enabled, interaction with the second Mn(2+) but did not result in enhancement in, potency. Introduction of a tertiary amino moiety at the ortho-position of, the sulfonyl phenyl ring gave reduced protein binding and improved, cellular activity, but led to lower oral bioavailability.

A series of aryl sulfonamides of 5,6-disubstituted anthranilic acids were identified as potent inhibitors of methionine aminopeptidase-2 (MetAP2). Small alkyl groups and 3-furyl were tolerated at the 5-position of anthranilic acid, while -OCH(3), CH(3), and Cl were found optimal for the 6-position. Placement of 2-aminoethoxy group at the 6-position enabled interaction with the second Mn(2+) but did not result in enhancement in potency. Introduction of a tertiary amino moiety at the ortho-position of the sulfonyl phenyl ring gave reduced protein binding and improved cellular activity, but led to lower oral bioavailability.

==About this Structure==

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[[Category: Methionyl aminopeptidase]]

[[Category: Single protein]]

[[Category: Park, C.H.]]

[[Category: Park, C H.]]

[[Category: F77]]

[[Category: MN]]

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[[Category: protein-ligand complex]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Wed~~ Feb ~~13 08~~:13:43 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:07:51 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
-A series of aryl sulfonamides of 5,6-disubstituted anthranilic acids were, identified as potent inhibitors of methionine aminopeptidase-2 (MetAP2)., Small alkyl groups and 3-furyl were tolerated at the 5-position of, anthranilic acid, while -OCH(3), CH(3), and Cl were found optimal for the, 6-position. Placement of 2-aminoethoxy group at the 6-position enabled, interaction with the second Mn(2+) but did not result in enhancement in, potency. Introduction of a tertiary amino moiety at the ortho-position of, the sulfonyl phenyl ring gave reduced protein binding and improved, cellular activity, but led to lower oral bioavailability.
+A series of aryl sulfonamides of 5,6-disubstituted anthranilic acids were identified as potent inhibitors of methionine aminopeptidase-2 (MetAP2). Small alkyl groups and 3-furyl were tolerated at the 5-position of anthranilic acid, while -OCH(3), CH(3), and Cl were found optimal for the 6-position. Placement of 2-aminoethoxy group at the 6-position enabled interaction with the second Mn(2+) but did not result in enhancement in potency. Introduction of a tertiary amino moiety at the ortho-position of the sulfonyl phenyl ring gave reduced protein binding and improved cellular activity, but led to lower oral bioavailability.
 ==About this Structure==
@@ Line 14: / Line 14: @@
 [[Category: Methionyl aminopeptidase]]
 [[Category: Single protein]]
-[[Category: Park, C.H.]]
+[[Category: Park, C H.]]
 [[Category: F77]]
 [[Category: MN]]
@@ Line 20: / Line 20: @@
 [[Category: protein-ligand complex]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 13 08:13:43 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:07:51 2008''