Photolabeling of tissue transglutaminase reveals the binding mode of potent cinnamoyl inhibitors.

@article{Pardin2009PhotolabelingOT,
  title={Photolabeling of tissue transglutaminase reveals the binding mode of potent cinnamoyl inhibitors.},
  author={Christophe Pardin and Isabelle Roy and Roberto A. Chica and Eric Bonneil and Pierre Thibault and William D Lubell and Joelle N Pelletier and Jeffrey W Keillor},
  journal={Biochemistry},
  year={2009},
  volume={48 15},
  pages={3346-53}
}
We have recently developed a new class of cinnamoyl derivatives as potent tissue transglutaminase (TG2) inhibitors. Herein, we report the synthesis of a diazirine derivative of these inhibitors and its application to the photolabeling of its binding site on guinea pig liver transglutaminase. Two novel homology models were generated for this commonly studied TG2, which differ in the conformational state they represent. Tryptic digest and mass spectrometric analysis of the photolabeling… CONTINUE READING