5′-O-去磷酸化 2′,5′-寡聚腺苷酸（2-5A）在 2′-末端带有 8-甲基腺苷，可激活人 RNase L。
5'-O-dephosphorylated 2',5'-oligoadenylate (2-5A) with 8-methyladenosine at the 2'-terminus activates human RNase L.
机构信息
United Graduate School of Drug Discovery and Medical Information Science, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1186-8. doi: 10.1016/j.bmcl.2009.12.005. Epub 2009 Dec 4.
Human ribonuclease L (RNase L), an interferon-induced endoribonuclease, becomes enzymatically active after binding to 2-5A. The 5'-phosphoryl group of 2-5A is reportedly necessary for the conformational change leading to RNase L activation. However, we found that 5'-O-dephosphorylated 2-5A tetramer analogs with 8-methyladenosine at the 2'-terminus were more effective as an activator of RNase L than the parent 2-5A tetramer. Introduction of 8-methyladenosine is thought to induce a dramatic shift of 2-5A in the binding site of RNase L.
人核糖核酸酶 L（RNase L）是一种干扰素诱导的内切核酸酶，在与 2-5A 结合后变得具有酶活性。据报道，2-5A 的 5'-磷酸基团对于导致 RNase L 激活的构象变化是必需的。然而，我们发现，在 2'-末端具有 8-甲基腺苷的 5'-去磷酸化 2-5A 四聚体类似物比母体 2-5A 四聚体更有效地作为 RNase L 的激活剂。引入 8-甲基腺苷被认为会诱导 2-5A 在 RNase L 结合位点上发生剧烈的位移。
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