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)

Res Commun Chem Pathol Pharmacol. 1980 Jan;27(1):175-82.

Abstract

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.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Antibiotics, Antineoplastic / pharmacology*
  • Cells, Cultured
  • Glycine / analogs & derivatives*
  • Glycine / pharmacology
  • Half-Life
  • Humans
  • Isoxazoles / pharmacology*
  • Oxazoles / pharmacology*
  • Pancreatic Neoplasms / enzymology*
  • Time Factors
  • gamma-Glutamyltransferase / antagonists & inhibitors*

Substances

  • Antibiotics, Antineoplastic
  • Isoxazoles
  • Oxazoles
  • gamma-Glutamyltransferase
  • acivicin
  • Glycine