Munich Center for Integrated Protein Science (CIPS-M).
Biochemistry. 2013 Dec 17;52(50):8972-4. doi: 10.1021/bi4014402. Epub 2013 Dec 6.
Incorporation of the azobenzene derivative gluazo, a synthetic photochromic ligand, into a kainate receptor allows for the optical control of neuronal activity. The crystal structure of gluazo bound to a dimeric GluK2 ligand-binding domain reveals one monomer in a closed conformation, occupied by gluazo, and the other in an open conformation, with a bound buffer molecule. The glutamate group of gluazo interacts like the natural glutamate ligand, while its trans-azobenzene moiety protrudes into a tunnel. This elongated cavity presumably cannot accommodate a cis-azobenzene, which explains the reversible activation of the receptor upon photoisomerization.
将合成光致变色配体偶氮苯衍生物 gluazo 掺入到 kainate 受体中，使得对神经元活动的光学控制成为可能。与二聚体 GluK2 配体结合域结合的 gluazo 的晶体结构显示，一个单体处于封闭构象，被 gluazo 占据，另一个处于开放构象，结合有缓冲分子。Gluazo 的谷氨酸基团与天然谷氨酸配体相互作用，而其反式偶氮苯部分突出到一个隧道中。这个拉长的腔推测不能容纳顺式偶氮苯，这解释了光致异构化时受体的可逆激活。
