Alexander Seth C, Schepartz Alanna
Department of Chemistry and ‡Department of Molecular, Cellular and Developmental Biology, Yale University , New Haven, Connecticut 06520-8107, United States.
Org Lett. 2014 Jul 18;16(14):3824-7. doi: 10.1021/ol501721j. Epub 2014 Jul 7.
There is great interest in fluorogenic compounds that tag biomolecules within cells. Biarsenicals are fluorogenic compounds that become fluorescent upon binding four proximal Cys thiols, a tetracysteine (Cys(4)) motif. This work details interactions between the biarsenical AsCy3 and Cys(4) peptides. Maximal affinity was observed when two Cys-Cys pairs were separated by at least 8 amino acids; the highest affinity ligand bound in the nanomolar concentration range (K(app) = 43 nM) and with a significant (3.2-fold) fluorescence enhancement.
人们对能够标记细胞内生物分子的荧光化合物有着浓厚的兴趣。双砷化合物是一类荧光化合物，它们在与四个相邻的半胱氨酸硫醇（一种四半胱氨酸（Cys(4)）基序）结合后会发出荧光。这项工作详细描述了双砷化合物AsCy3与Cys(4)肽之间的相互作用。当两个半胱氨酸-半胱氨酸对被至少8个氨基酸隔开时，观察到最大亲和力；亲和力最高的配体在纳摩尔浓度范围内结合（K(app)=43 nM），并且荧光有显著增强（3.2倍）。
