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Literature summary extracted from

  • Pardin, C.; Roy, I.; Chica, R.A.; Bonneil, E.; Thibault, P.; Lubell, W.D.; Pelletier, J.N.; Keillor, J.W.
    Photolabeling of tissue transglutaminase reveals the binding mode of potent cinnamoyl inhibitors (2009), Biochemistry, 48, 3346-3353.
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.3.2.13 homology modeling of enzyme photolabeled by 3-(3-methyl-3H-diaziren-3-yl)-N-[4-[(1E)-3-oxo-3-(pyridin-3-yl)prop-1-en-1-yl]phenyl]propanamide. In the closed conformation of enzyme, C230 is more solvent-exposed than in the open conformation. Docking experiments suggest binding modes that block access to the tunnel leading to the active site Cavia porcellus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.2.13 3-(3-methyl-3H-diaziren-3-yl)-N-[4-[(1E)-3-oxo-3-(pyridin-3-yl)prop-1-en-1-yl]phenyl]propanamide reversible inhibitor and photolabel. In labeling experiments, specific labeling of residue C230 Cavia porcellus

Organism

EC Number Organism UniProt Comment Textmining
2.3.2.13 Cavia porcellus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.2.13 liver
-
 Cavia porcellus
-

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.2.13 0.028
-
 pH 7.0, 25°C Cavia porcellus 3-(3-methyl-3H-diaziren-3-yl)-N-[4-[(1E)-3-oxo-3-(pyridin-3-yl)prop-1-en-1-yl]phenyl]propanamide