Abstract:
In this issue of Structure, Chi et al.1 report structural and functional studies that reveal the inhibition mechanism of the lysosomal two-pore channel TPC2 by the antagonist SG-094, which is of interest for drug development. Antagonist binding induces the downward displacement of the voltage-sensor domain II (VSD II), which is accompanied by asymmetric conformational rearrangements of the entire channel.
摘要:
在本期的结构中,Chi等人1报道了结构和功能研究,揭示了拮抗剂SG-094对溶酶体两孔通道TPC2的抑制机制,这对药物开发很有意义。拮抗剂结合诱导电压传感器域II(VSDII)的向下位移,伴随着整个通道的不对称构象重排。