Trads Julie B, Burgstaller Jessica, Laprell Laura, Konrad David B, de la Osa de la Rosa Luis, Weaver C David, Baier Herwig, Trauner Dirk, Barber David M
Department of Chemistry and Center for Integrated Protein Science, Ludwig Maximilians University Munich, Butenandtstraße 5-13, 81377 Munich, Germany.
Max Planck Institute of Neurobiology, Am Klopferspitz 18, 82152 Martinsried, Germany.
Org Biomol Chem. 2016 Dec 20;15(1):76-81. doi: 10.1039/c6ob02153k.
G-protein coupled inwardly rectifying potassium (GIRK) channels are an integral part of inhibitory signal transduction pathways, reducing the activity of excitable cells via hyperpolarization. They play crucial roles in processes such as cardiac output, cognition and the coordination of movement. Therefore, the precision control of GIRK channels is of critical importance. Here, we describe the development of the azobenzene containing molecule VLOGO (Visible Light Operated GIRK channel Opener), which activates GIRK channels in the dark and is promptly deactivated when illuminated with green light. VLOGO is a valuable addition to the existing tools for the optical control of GIRK channels as it circumvents the need to use potentially harmful UV irradiation. We therefore believe that VLOGO will be a useful research tool for studying GIRK channels in biological systems.
G蛋白偶联内向整流钾通道(GIRK通道)是抑制性信号转导通路的一个组成部分,通过超极化降低可兴奋细胞的活性。它们在诸如心输出量、认知和运动协调等过程中发挥着关键作用。因此,精确控制GIRK通道至关重要。在此,我们描述了含偶氮苯分子VLOGO(可见光操作的GIRK通道开放剂)的开发,该分子在黑暗中激活GIRK通道,并在绿光照射下迅速失活。VLOGO是现有用于光控GIRK通道的工具的一个有价值的补充,因为它避免了使用可能有害的紫外线照射的需要。因此,我们相信VLOGO将成为研究生物系统中GIRK通道的有用研究工具。