Evaluation of novel dipeptide-bound alpha,beta-unsaturated amides and epoxides as irreversible inhibitors of guinea pig liver transglutaminase.
Herein, we report the results of irreversible inhibition of guinea pig liver transglutaminase (TGase) by a series of 24 novel dipeptides containing either an alpha,beta-unsaturated amide or an epoxide functional group. Their inactivation rate constants were measured using a direct continuous spectrophotometric method and were found to vary between 421 x 10(3) and 3000 x 10(3)M(-1)min(-1).
Marrano
C
C
Département de chimie, Université de Montréal, C.P. 6128, Succursale centre-ville, Montréal, Québec, Canada H3C 3J7.
de Macédo
P
P
Keillor
J W
JW
D000577:Amides / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004852:Epoxy Compounds / Q000737:chemistry / Q000494:pharmacology*; D006168:Guinea Pigs; D007700:Kinetics; D008099:Liver / Q000187:drug effects* / Q000201:enzymology; D009682:Magnetic Resonance Spectroscopy; D011503:Transglutaminases / Q000037:antagonists & inhibitors*
D000577:Amides; D004791:Enzyme Inhibitors; D004852:Epoxy Compounds; D011503:Transglutaminases