2ea2: Difference between revisions

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[[Image:2ea2.jpg|left|200px]]
{{Seed}}
[[Image:2ea2.png|left|200px]]


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{{STRUCTURE_2ea2|  PDB=2ea2  |  SCENE=  }}  
{{STRUCTURE_2ea2|  PDB=2ea2  |  SCENE=  }}  


'''h-MetAP2 complexed with A773812'''
===h-MetAP2 complexed with A773812===




==Overview==
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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.
The line below this paragraph, {{ABSTRACT_PUBMED_17350258}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 17350258 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17350258}}


==About this Structure==
==About this Structure==
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[[Category: Hydrolase]]
[[Category: Hydrolase]]
[[Category: Protein-ligand complex]]
[[Category: Protein-ligand complex]]
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