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[新型5'-硫化核苷作为多胺生物合成的抑制剂]

[New 5'-sulfurated nucleosides as inhibitors of the biosynthesis of polyamines].

作者信息

Cacciapuoti G, Porcelli M, Della Ragione F, Pontoni G, Cartenì-Farina M

出版信息

Boll Soc Ital Biol Sper. 1980 Feb 15;56(3):238-44.

PMID:6989378
Abstract

The inhibitory effect of the deaminated analogs of S-adenosyl(5')-3-methylthiopropylamine on spermidine synthase (EC 2.5.1.16.) from E. coli, AdoMet decarboxylase (EC 4.1.1.50.) from human placenta and E. coli and AdoMet lyase (EC 3.3.1.-) from rat liver have been reported. 5'-isobutylthioadenosine, a new powerful antiproliferative drug has been assayed as substrate of MTA phosphorylase (EC 2.4.2.1). The apparent Km is 1,8x10(-5) M. The inhibitory effect of 5'-isobutylthiadenosine on AdoMet lyase and spermidine synthase was also demonstrated.

摘要

已报道了S-腺苷基(5')-3-甲基硫丙胺的脱氨基类似物对来自大肠杆菌的亚精胺合酶(EC 2.5.1.16.)、来自人胎盘和大肠杆菌的腺苷甲硫氨酸脱羧酶(EC 4.1.1.50.)以及来自大鼠肝脏的腺苷甲硫氨酸裂解酶(EC 3.3.1.-)的抑制作用。5'-异丁硫基腺苷是一种新型强效抗增殖药物,已被测定为MTA磷酸化酶(EC 2.4.2.1)的底物。其表观Km为1.8×10(-5) M。还证实了5'-异丁硫基腺苷对腺苷甲硫氨酸裂解酶和亚精胺合酶的抑制作用。

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