CC chemokine receptor 4（CCR4） is a G-protein-coupled receptor which plays a pivotal role in allergic inflammation. In the present study, three extracellular loops（EL1-3） of CCR4 were synthesized, and the interacti...
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CC chemokine receptor 4（CCR4） is a G-protein-coupled receptor which plays a pivotal role in allergic inflammation. In the present study, three extracellular loops（EL1-3） of CCR4 were synthesized, and the interactions between the extracellular loops and compound S009 were investigated using capillary zone electrophoresis（CZE）. Both qualitative and quantitative characterizations of the compound-peptide binding were carried out. The experimental data indicated that compound S009 exhibited interactions with EL3, and a binding constant of（12.5±0.19）×10^4 M^-1 was determined using the Scatchard plot. Our study identified the specific domains of CCR4 that could be targeted by small molecules and provided insights for the discovery of novel CCR4 antagonists.
研究背景:低密度脂蛋白受体相关蛋白4(low-density lipoprotein receptor-related protein 4,LRP4)是存在于神经肌肉接头处(NMJ)突触后膜上的跨膜蛋白质.聚集蛋白(Agrin)从运动神经元末梢释放,与LRP4结合并激活肌肉特异性激酶(MuSK),磷...
详细信息
研究背景:低密度脂蛋白受体相关蛋白4(low-density lipoprotein receptor-related protein 4,LRP4)是存在于神经肌肉接头处(NMJ)突触后膜上的跨膜蛋白质.聚集蛋白(Agrin)从运动神经元末梢释放,与LRP4结合并激活肌肉特异性激酶(MuSK),磷酸化的MuSK蛋白触发了受体相关蛋白(rapsyn)并诱导了乙酰胆碱受体(AChR)的聚集,形成了NMJ突触后膜的作用机制.LRP4作为聚集蛋白的受体对MuSK的激活,AChR的聚集以及维持NMJ的结构起重要作用.
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