Inhibition of uridine phosphorylase from Escherichia coli by benzylacyclouridines.
Inhibition of uridine phosphorylase from Escherichia coli by benzylacyclouridines.
复制标题
苄基环尿苷对大肠杆菌尿苷磷酸化酶的抑制。
DOI：
10.1016/0006-2952(86)90675-1
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发表时间：
1986
影响因子：
5.8
通讯作者：
Cha,S
中科院分区：
文献类型：
--
作者：
Park,KS;elKouni,MH;Krenitsky,TA;Chu,SH;Cha,S
研究发现，哺乳动物尿苷磷酸化酶的强效和特异性的抑制剂--苄基丙烯酸类化合物也能抑制大肠杆菌的尿苷磷酸化酶，但不能抑制胸苷磷酸化酶。在所有情况下都观察到竞争抑制，这些化合物中最有效的是HM-BBAU(5-(3-benzyloxybenzyl)-1-[(2′-hydroxy-1′-hydroxymethyl)methyl]uracil)，Ki值为0.15BBAU M。这些化合物的抑制能力与从哺乳动物来源的酶获得的抑制能力相当[Niedzwickiet al.，Biochem]。Pharmac.31,1857(1982)和Naguibet等人，手稿正在准备中]表明尿苷磷酸化酶的活性部位的结构来自。Colimay类似于哺乳动物的酶。
The benzylacyclouridines, potent and specific inhibitors of mammalian uridine phosphorylase, were also found to be inhibitors of uridine phosphorylase but not thymidine phosphorylase fromEscherichia coli. Competitive inhibition was observed in all cases and the most potent of these compounds was HM-BBAU (5-(3-benzyloxybenzyl)-1-[(2′-hydroxy-1′-hydroxymethyl)methyl]uracil) with aKivalue of 0.15 μM. The inhibitory potencies of these compounds parallel those obtained with enzymes from mammalian sources [Niedzwickiet al., Biochem. Pharmac.31, 1857 (1982) and Naguibet al., manuscript in preparation] indicating that the structure of the active site of uridine phosphorylase fromE. colimay resemble that of the mammalian enzyme.