MacKinnon R, Cohen S L, Kuo A, Lee A, Chait B T
Laboratory of Molecular Neurobiology and Biophysics and the Howard Hughes Medical Institute, Rockefeller University, 1230 York Avenue, New York, NY 10021, USA.
Science. 1998 Apr 3;280(5360):106-9. doi: 10.1126/science.280.5360.106.
Toxins from scorpion venom interact with potassium channels. Resin-attached, mutant K+ channels from Streptomyces lividans were used to screen venom from Leiurus quinquestriatus hebraeus, and the toxins that interacted with the channel were rapidly identified by mass spectrometry. One of the toxins, agitoxin2, was further studied by mutagenesis and radioligand binding. The results show that a prokaryotic K+ channel has the same pore structure as eukaryotic K+ channels. This structural conservation, through application of techniques presented here, offers a new approach for K+ channel pharmacology.
蝎毒中的毒素与钾通道相互作用。利用来自淡青链霉菌的树脂附着型突变钾离子通道筛选以色列金蝎的毒液，并通过质谱法快速鉴定出与该通道相互作用的毒素。其中一种毒素，即激动毒素2，通过诱变和放射性配体结合进行了进一步研究。结果表明，原核钾离子通道与真核钾离子通道具有相同的孔结构。通过应用本文介绍的技术，这种结构上的保守性为钾通道药理学提供了一种新方法。
