肌醇衍生物作为 D-手性肌醇 1,4,5-三磷酸受体拮抗剂的研究进展。
Development of inositol-based antagonists for the D-myo-inositol 1,4,5-trisphosphate receptor.
机构信息
School of Chemistry and Centre for Biomolecular Sciences, University of St Andrews, North Haugh, St Andrews, Fife, KY16 9ST, UK.
出版信息
Chem Commun (Camb). 2011 Jan 7;47(1):242-4. doi: 10.1039/c0cc03003a. Epub 2010 Oct 11.
PMID:20938532
Abstract
The syntheses of four D-myo-inositol 1,4,5-trisphosphate (InsP(3)) derivatives, incorporating phosphate bioisosteres at the 5-position, are reported. The methyl phosphate ester and sulfate derivatives retain InsP(3) receptor (InsP(3)R) agonist activity; the compounds that possess a methylphosphonate or a carboxymethyl moiety are InsP(3)R antagonists.
摘要
报道了四种 D-肌醇 1,4,5-三磷酸（InsP(3)）衍生物的合成，这些衍生物在 5 位引入了磷酸生物等排体。甲基磷酸酯和硫酸酯衍生物保留了 InsP(3)受体（InsP(3)R）激动剂活性；而具有甲基膦酸酯或羧甲基部分的化合物则是 InsP(3)R 拮抗剂。
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