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 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.