Aptameric inhibition of p210bcr-abl tyrosine kinase autophosphorylation by oligodeoxynucleotides of defined sequence and backbone structure.
Aptameric inhibition of p210bcr-abl tyrosine kinase autophosphorylation by oligodeoxynucleotides of defined sequence and backbone structure.
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通过具有确定序列和骨架结构的寡脱氧核苷酸对 p210bcr-abl 酪氨酸激酶自磷酸化的适体抑制。
作者：
Raymond C. Bergan;Y. Connell;Brigid Fahmy;E. Kyle;Len Neckers
蛋白酪氨酸激酶在细胞生理学中起关键作用。这些酶的特异性抑制剂是重要的实验室工具，并可能被证明是新的治疗剂。在这份报告中，我们描述了一类新的酪氨酸激酶抑制剂，合成寡脱氧核苷酸（ODNs）。描述了一种ODN，其在体外特异性抑制p210 bcr-abl酪氨酸激酶自磷酸化，Ki为0.5 μ M。相对于ATP，抑制是非竞争性的。ODN结构修饰对抑制活性的影响。所描述的抑制作用不是由经典的反义机制介导的，并且代表了最近认识到的ODN适体特性的一个例子。
Protein tyrosine kinases play key roles in cellular physiology. Specific inhibitors of these enzymes are important laboratory tools and may prove to be novel therapeutic agents. In this report we describe a new class of tyrosine kinase inhibitor, synthetic oligodeoxynucleotides (ODNs). An ODN is described which specifically inhibits p210bcr-abl tyrosine kinase autophosphorylation in vitro with a Ki of 0.5 microM. Inhibition is non-competitive with respect to ATP. The effects upon inhibitory activity of ODN structure modifications are described. The inhibition described is not mediated by classical antisense mechanisms and represents an example of the recently recognized aptameric properties of ODNs.