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Literature summary for 5.4.2.11 extracted from

  • Evans, M.J.; Morris, G.M.; Wu, J.; Olson, A.J.; Sorensen, E.J.; Cravatt, B.F.
    Mechanistic and structural requirements for active site labeling of phosphoglycerate mutase by spiroepoxides (2007), Mol. Biosyst., 3, 495-506.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
modeling study of enzyme in complex with inhibitor 1-benzyl 4-[(3R,4R,6R)-6-[1-(hex-5-ynoyloxy)-1-methylethyl]-1-oxaspiro[2.5]oct-4-yl] (2R)-2-(2,3-dihydro-1H-indol-3-ylmethyl)butanedioate Homo sapiens

Protein Variants

Protein Variants Comment Organism
K100A no covalent modification by inhibitor 1-benzyl 4-[(3R,4R,6R)-6-[1-(hex-5-ynoyloxy)-1-methylethyl]-1-oxaspiro[2.5]oct-4-yl] (2R)-2-(2,3-dihydro-1H-indol-3-ylmethyl)butanedioate Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-benzyl 4-[(3R,4R,6R)-6-[1-(hex-5-ynoyloxy)-1-methylethyl]-1-oxaspiro[2.5]oct-4-yl] (2R)-2-(2,3-dihydro-1H-indol-3-ylmethyl)butanedioate i.e. MJE3, spiroepoxide with anti-proliferative effects in human breast cancer cells. MJE3 covalently inactiviates enzyme at K100 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P18669
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