Design and characterization of mechanism-based inhibitors for the tyrosine aminomutase SgTAM.
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Montavon TJ, Christianson CV, Festin GM, Shen B, Bruner SD
Design and characterization of mechanism-based inhibitors for the tyrosine aminomutase SgTAM.
Bioorg Med Chem Lett. 2008 May 15;18(10):3099-102. Epub 2007 Nov 19.
- PubMed ID
- 18078753 [ View in PubMed]
- Abstract
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.