2rjs: Difference between revisions
New page: left|200px<br /><applet load="2rjs" size="350" color="white" frame="true" align="right" spinBox="true" caption="2rjs, resolution 2.400Å" /> '''SgTAM bound to subs... |
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==Overview== | ==Overview== | ||
The synthesis and evaluation of two classes of inhibitors for SgTAM, a | The synthesis and evaluation of two classes of inhibitors for SgTAM, a 4-methylideneimidazole-5-one (MIO) containing tyrosine aminomutase, are described. A mechanism-based strategy was used to design analogs that mimic the substrate or product of the reaction and form covalent interactions with the enzyme through the MIO prosthetic group. The analogs were characterized by measuring inhibition constants and X-ray crystallographic structural analysis of the co-complexes bound to the aminomutase, SgTAM. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Streptomyces globisporus]] | [[Category: Streptomyces globisporus]] | ||
[[Category: Tyrosine 2,3-aminomutase]] | [[Category: Tyrosine 2,3-aminomutase]] | ||
[[Category: Bruner, S | [[Category: Bruner, S D.]] | ||
[[Category: Christianson, C | [[Category: Christianson, C V.]] | ||
[[Category: Montavon, T | [[Category: Montavon, T J.]] | ||
[[Category: 296]] | [[Category: 296]] | ||
[[Category: 4-methylidene imidazole]] | [[Category: 4-methylidene imidazole]] | ||
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[[Category: mio]] | [[Category: mio]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:47:57 2008'' | ||
Revision as of 19:47, 21 February 2008
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SgTAM bound to substrate mimic
OverviewOverview
The synthesis and evaluation of two classes of inhibitors for SgTAM, a 4-methylideneimidazole-5-one (MIO) containing tyrosine aminomutase, are described. A mechanism-based strategy was used to design analogs that mimic the substrate or product of the reaction and form covalent interactions with the enzyme through the MIO prosthetic group. The analogs were characterized by measuring inhibition constants and X-ray crystallographic structural analysis of the co-complexes bound to the aminomutase, SgTAM.
About this StructureAbout this Structure
2RJS is a Single protein structure of sequence from Streptomyces globisporus with as ligand. Active as Tyrosine 2,3-aminomutase, with EC number 5.4.3.6 Full crystallographic information is available from OCA.
ReferenceReference
Design and characterization of mechanism-based inhibitors for the tyrosine aminomutase SgTAM., Montavon TJ, Christianson CV, Festin GM, Shen B, Bruner SD, Bioorg Med Chem Lett. 2007 Nov 19;. PMID:18078753
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