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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).
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1980
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Mia Paca-2Pancreatic CancerBiochemistryAlpha S,5sMedicineAlpha S-Alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic AcidNatural SciencesGamma-glutamyl TranspeptidaseOncogenic AgentInactivation Half-lifeAnti-cancer AgentCellular BiochemistryPharmacologyCancer ResearchTumor BiologyGlycosylation
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.