2RJS
SgTAM bound to substrate mimic
Summary for 2RJS
Entry DOI | 10.2210/pdb2rjs/pdb |
Related | 2OHY 2QVE 2RJR |
Descriptor | Tyrosine aminomutase, (3R)-3-amino-2,2-difluoro-3-(4-methoxyphenyl)propanoic acid (3 entities in total) |
Functional Keywords | 4-methylidene imidazole, mio, aminomutase, c-1027, isomerase |
Biological source | Streptomyces globisporus |
Total number of polymer chains | 2 |
Total formula weight | 116799.92 |
Authors | Montavon, T.J.,Christianson, C.V.,Bruner, S.D. (deposition date: 2007-10-15, release date: 2008-01-15, Last modification date: 2024-10-30) |
Primary citation | Montavon, T.J.,Christianson, C.V.,Festin, G.M.,Shen, B.,Bruner, S.D. Design and characterization of mechanism-based inhibitors for the tyrosine aminomutase SgTAM. Bioorg.Med.Chem.Lett., 18:3099-3102, 2008 Cited by 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. PubMed: 18078753DOI: 10.1016/j.bmcl.2007.11.046 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.4 Å) |
Structure validation
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