1boa: Difference between revisions

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==Overview==

The fungal metabolite fumagillin suppresses the formation of new blood, vessels, and a fumagillin analog is currently in clinical trials as an, anticancer agent. The molecular target of fumagillin is methionine, aminopeptidase-2 (MetAP-2). A 1.8 A resolution crystal structure of free, and inhibited human MetAP-2 shows a covalent bond formed between a, reactive epoxide of fumagillin and histidine-231 in the active site of, MetAP-2. Extensive hydrophobic and water-mediated polar interactions with, other parts of fumagillin provide additional affinity. Fumagillin-based, drugs inhibit MetAP-2 but not MetAP-1, and the three-dimensional structure, also indicates the likely determinants of this specificity. The structural, basis for fumagillin's potency and specificity forms the starting point, for structure-based drug design.

The fungal metabolite fumagillin suppresses the formation of new blood vessels, and a fumagillin analog is currently in clinical trials as an anticancer agent. The molecular target of fumagillin is methionine aminopeptidase-2 (MetAP-2). A 1.8 A resolution crystal structure of free and inhibited human MetAP-2 shows a covalent bond formed between a reactive epoxide of fumagillin and histidine-231 in the active site of MetAP-2. Extensive hydrophobic and water-mediated polar interactions with other parts of fumagillin provide additional affinity. Fumagillin-based drugs inhibit MetAP-2 but not MetAP-1, and the three-dimensional structure also indicates the likely determinants of this specificity. The structural basis for fumagillin's potency and specificity forms the starting point for structure-based drug design.

==About this Structure==

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[[Category: Methionyl aminopeptidase]]

[[Category: Single protein]]

[[Category: Clardy, J.C.]]

[[Category: Clardy, J C.]]

[[Category: Crews, C.M.]]

[[Category: Crews, C M.]]

[[Category: Kemp, C.W.]]

[[Category: Kemp, C W.]]

[[Category: Liu, S.]]

[[Category: Widom, J.]]

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[[Category: methionine aminopeptidase]]

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@@ Line 4: / Line 4: @@
 ==Overview==
-The fungal metabolite fumagillin suppresses the formation of new blood, vessels, and a fumagillin analog is currently in clinical trials as an, anticancer agent. The molecular target of fumagillin is methionine, aminopeptidase-2 (MetAP-2). A 1.8 A resolution crystal structure of free, and inhibited human MetAP-2 shows a covalent bond formed between a, reactive epoxide of fumagillin and histidine-231 in the active site of, MetAP-2. Extensive hydrophobic and water-mediated polar interactions with, other parts of fumagillin provide additional affinity. Fumagillin-based, drugs inhibit MetAP-2 but not MetAP-1, and the three-dimensional structure, also indicates the likely determinants of this specificity. The structural, basis for fumagillin's potency and specificity forms the starting point, for structure-based drug design.
+The fungal metabolite fumagillin suppresses the formation of new blood vessels, and a fumagillin analog is currently in clinical trials as an anticancer agent. The molecular target of fumagillin is methionine aminopeptidase-2 (MetAP-2). A 1.8 A resolution crystal structure of free and inhibited human MetAP-2 shows a covalent bond formed between a reactive epoxide of fumagillin and histidine-231 in the active site of MetAP-2. Extensive hydrophobic and water-mediated polar interactions with other parts of fumagillin provide additional affinity. Fumagillin-based drugs inhibit MetAP-2 but not MetAP-1, and the three-dimensional structure also indicates the likely determinants of this specificity. The structural basis for fumagillin's potency and specificity forms the starting point for structure-based drug design.
 ==About this Structure==
@@ Line 14: / Line 14: @@
 [[Category: Methionyl aminopeptidase]]
 [[Category: Single protein]]
-[[Category: Clardy, J.C.]]
+[[Category: Clardy, J C.]]
-[[Category: Crews, C.M.]]
+[[Category: Crews, C M.]]
-[[Category: Kemp, C.W.]]
+[[Category: Kemp, C W.]]
 [[Category: Liu, S.]]
 [[Category: Widom, J.]]
@@ Line 26: / Line 26: @@
 [[Category: methionine aminopeptidase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb  3 09:33:28 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 11:57:24 2008''