Riley Andrew M, Wang Huanchen, Shears Stephen B, L Potter Barry V
Wolfson Laboratory of Medicinal Chemistry, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK.
Chem Commun (Camb). 2015 Aug 14;51(63):12605-8. doi: 10.1039/c5cc05017k.
To synthesise stabilised mimics of InsP8, the most phosphorylated inositol phosphate signalling molecule in Nature, we replaced its two diphosphate (PP) groups with either phosphonoacetate (PA) or methylenebisphosphonate (PCP) groups. Utility of the PA and PCP analogues was verified by structural and biochemical analyses of their interactions with enzymes of InsP8 metabolism.
为了合成自然界中磷酸化程度最高的肌醇磷酸信号分子InsP8的稳定模拟物,我们用膦酰基乙酸(PA)或亚甲基双膦酸酯(PCP)基团取代了它的两个二磷酸(PP)基团。通过对PA和PCP类似物与InsP8代谢酶相互作用的结构和生化分析,验证了它们的效用。