Tissue transglutaminase inhibition.
Khosla and coworkers report the synthesis of peptidic dihydroisoxazole derivatives, the in vitro evaluation of these novel compounds as inhibitors of recombinant human tissue transglutaminase (TG2), and their oral bioavailability and efficacy for the synergistic treatment of glioblastoma tumors.
Keillor
Jeffrey W
JW
Départment de Chimie, Université de Montréal, Québec H3C 3J7, Canada.
D000818:Animals; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D011485:Protein Binding; D011994:Recombinant Proteins; D013329:Structure-Activity Relationship; D011503:Transglutaminases / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D011994:Recombinant Proteins; D011503:Transglutaminases