首个二磷酸肌醇多磷酸盐的合成类似物：与 PP-InsP5 激酶的相互作用。
First synthetic analogues of diphosphoinositol polyphosphates: interaction with PP-InsP5 kinase.
机构信息
Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, BA2 7AY, UK.
出版信息
Chem Commun (Camb). 2012 Nov 28;48(92):11292-4. doi: 10.1039/c2cc36044f.
Abstract
We synthesised analogues of diphosphoinositol polyphosphates (PP-InsPs) in which the diphosphate is replaced by an α-phosphonoacetic acid (PA) ester. Structural analysis revealed that 5-PA-InsP(5) mimics 5-PP-InsP(5) binding to the kinase domain of PPIP5K2; both molecules were phosphorylated by the enzyme. PA-InsPs are promising candidates for further studies into the biology of PP-InsPs.
摘要
我们合成了二磷酸肌醇多磷酸盐（PP-InsPs）的类似物，其中二磷酸酯被α-膦酸乙酸（PA）酯取代。结构分析表明，5-PA-InsP（5）模拟 5-PP-InsP（5）与 PPIP5K2 激酶结构域的结合；两种分子均被该酶磷酸化。PA-InsPs 是进一步研究 PP-InsPs 生物学的有前途的候选物。
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