The inhibition of gamma-glutamyl transpeptidase from human pancreatic carcinoma cells by (alpha S,5S)-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid (AT-125; NSC-163501).
AT-125, (alpha S, 5S)-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid, at a concentration of 5 microM was found to inhibit the growth of human pancreatic carcinoma cells (MIA PaCa-2) by 78% after 72 hours in continuous culture. It was found that MIA PaCa-2 gamma-glutamyl transpeptidase (10 nmol/min/10(6) cells) was irreversibly inactivated by AT-125 with an inactivation half-life of 80 minutes at 450 microM.
D000903:Antibiotics, Antineoplastic / Q000494:pharmacology*; D002478:Cells, Cultured; D005998:Glycine / Q000031:analogs & derivatives* / Q000494:pharmacology; D006207:Half-Life; D006801:Humans; D007555:Isoxazoles / Q000494:pharmacology*; D010080:Oxazoles / Q000494:pharmacology*; D010190:Pancreatic Neoplasms / Q000201:enzymology*; D013997:Time Factors; D005723:gamma-Glutamyltransferase / Q000037:antagonists & inhibitors*
D000903:Antibiotics, Antineoplastic; D007555:Isoxazoles; D010080:Oxazoles; D005723:gamma-Glutamyltransferase; C006303:acivicin; D005998:Glycine