(αS,5S)-α-氨基-3-氯-4,5-二氢-5-异恶唑乙酸（AT-125；NSC-163501）对人胰腺癌细胞γ-谷氨酰转肽酶的抑制作用
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).
作者信息
Allen L, Meck R, Yunis A
出版信息
Res Commun Chem Pathol Pharmacol. 1980 Jan;27(1):175-82.
PMID:6102405
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.
摘要
AT - 125，即(αS, 5S)-α-氨基-3-氯-4,5-二氢-5-异恶唑乙酸，在连续培养72小时后，浓度为5微摩尔时可使人类胰腺癌细胞（MIA PaCa - 2）的生长抑制78%。研究发现，MIA PaCa - 2γ-谷氨酰转肽酶（10纳摩尔/分钟/10⁶个细胞）在450微摩尔的AT - 125作用下会不可逆失活，失活半衰期在450微摩尔时为80分钟。
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