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CC趋化因子受体4(CCR4)是G蛋白偶联受体的一种,在过敏性炎症中起着举足轻重的作用。在本研究中,我们合成了CCR4的三个胞外loop区(EL1–EL3),用毛细管区带电泳(CZE)的方法研究化合物S009和3个胞外loop区的相互作用。分别进行了定性和定量研究。实验数据表明,化合物S009和EL3有相互作用并通过Scatchard方程计算得到化合物S009和EL3之间的结合常数为(12.5±0.19)×104 M–1。我们的研究确证了CCR4结合小分子的具体胞外域并为进一步发现新型CCR4拮抗剂提供了有帮助的信息。
CC chemokine receptor 4 (CCR4) is a G protein-coupled receptor that plays a pivotal role in allergic inflammation. In this study, we synthesized three extracellular loop regions (EL1-EL3) of CCR4 and studied the interaction of compound S009 with three extracellular loop regions by capillary zone electrophoresis (CZE). Respectively, qualitative and quantitative research. Experimental data show that there is interaction between compound S009 and EL3 and the binding constant between compound S009 and EL3 is (12.5 ± 0.19) × 104 M-1 calculated by the Scatchard equation. Our study confirms the specific extracellular domain of CCR4 binding small molecule and provides helpful information for further discovery of novel CCR4 antagonists.