Development and application of "artificial biotin" derivatives using methodologies of chemical biology

为了进一步完善生物素-链霉亲和素作为化学生物学通用结合对的体系，我们筛选了约16万个化合物作为链霉亲和素的新型配体。结果，我们成功地获得了与蛋白质亲和在1 μM量级的新配体。此外，我们还通过x射线晶体学和计算机模拟分析了它们的结合机制。

In order to further sophisticate biotin-streptavidin system that is used as a universal binding pair in chemical biology, we screened a large library of approximately 160,000 compounds for novel ligands to streptavidin. As a result, we succeeded in obtaining new ligands that have affinities to the protein in the order of 1 μM. Moreover, we analyzed their binding mechanisms in detail by X-ray crystallography and computer simulation.