5'-（6-氨基嘌呤-9-基）-5'-脱氧-β-D-呋喃核糖苷2'，3'-环单磷酸甲酯：一种新型的、具有生物活性的环磷酸腺苷结构类似物。
Methyl 5'-(6-aminopurin-9-yl)-5'-deoxy-beta-D-ribofuranoside 2',3'-cyclic monophosphate: a novel, biologically active, structural analogue of cyclic AMP.
作者信息
Nair V, Wiechert R J, Vietti D E, Singh D, Stevens R H
出版信息
J Cyclic Nucleotide Res. 1980;6(3):189-200.
PMID:6255019
Abstract
A novel structural analogue of cyclic AMP has been synthesized. This compound has been found to activate protein kinase from skeletal muscle (Ka 5.0 microM). It is virtually resistant to degradation by beef heart cAMP phosphodiesterase. It is an inhibitor of this enzyme with an [I]50 of 47.0 microM. The proliferation of cancer cells (HT-29) is inhibited by this compound. It represents the first example of a 2',3'-cyclic nucleotide with marked biological activity.
摘要
一种新型的环磷酸腺苷结构类似物已被合成。已发现该化合物可激活骨骼肌中的蛋白激酶（Ka为5.0微摩尔）。它几乎对牛心环磷酸腺苷磷酸二酯酶的降解具有抗性。它是该酶的抑制剂，半数抑制浓度（[I]50）为47.0微摩尔。该化合物可抑制癌细胞（HT - 29）的增殖。它代表了具有显著生物活性的2',3'-环核苷酸的首个实例。
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