Danzin C, Casara P, Claverie N, Metcalf B W
J Med Chem. 1981 Jan;24(1):16-20. doi: 10.1021/jm00133a005.
alpha-Ethynyl- and alpha-vinylornithine were designed and synthesized as potential enzyme-activated inhibitors of mammalian ornithine decarboxylase. These two new inhibitors produce both immediate and time-dependent inhibition of rat liver ornithine decarboxylase in vitro. The inhibitions exhibition saturation kinetics. The apparent dissociation constants (KI) are 10 and 810 microM, and the times of half-inactivation at infinite concentration of inhibitor (t1/2) are 8.5 and 27 min, respectively, for alpha-ethynyl- and alpha-vinylornithine. In rats, alpha-ethynylornithine causes a rapid dose-dependent decrease of ornithine decarboxylase activity in prostate and, to a lesser extent, in thymus and testis.
α-乙炔基鸟氨酸和α-乙烯基鸟氨酸被设计并合成出来，作为哺乳动物鸟氨酸脱羧酶潜在的酶激活抑制剂。这两种新抑制剂在体外对大鼠肝脏鸟氨酸脱羧酶产生即时和时间依赖性抑制。抑制作用呈现饱和动力学。α-乙炔基鸟氨酸和α-乙烯基鸟氨酸的表观解离常数（KI）分别为10和810微摩尔，在抑制剂无限浓度下的半失活时间（t1/2）分别为8.5和27分钟。在大鼠中，α-乙炔基鸟氨酸会使前列腺中鸟氨酸脱羧酶活性迅速出现剂量依赖性下降，在胸腺和睾丸中下降程度较小。
