Biomics Laboratory, Institut de Recherches en Technologies et Sciences pour le Vivant, CEA, 17 rue des Martyrs, 38054 Grenoble, France.
J Am Chem Soc. 2011 Jul 6;133(26):10058-61. doi: 10.1021/ja204016e. Epub 2011 Jun 14.
Fluorescence imaging in clinical diagnostics and biomedical research relies to a great extent on the use of small organic fluorescent probes. Because of the difficulty of combining fluorescent and molecular-recognition properties, the development of such probes has been severely restricted to a number of well-known fluorescent scaffolds. Here we demonstrate that autofluorescing druglike molecules are a valuable source of bioimaging probes. Combinatorial synthesis and screening of chemical libraries in droplet microarrays allowed the identification of new types of fluorophores. Their concise and clean assembly by a multicomponent reaction presents a unique potential for the one-step synthesis of thousands of structurally diverse fluorescent molecules. Because they are based upon a druglike scaffold, these fluorophores retain their molecular recognition potential and can be used to design specific imaging probes.
荧光成像是临床诊断和生物医学研究中的一个重要手段，在很大程度上依赖于小分子有机荧光探针的使用。由于将荧光性质和分子识别性质结合在一起存在困难，此类探针的发展受到了很大限制，只能使用少数几种知名的荧光骨架。在这里，我们证明自发荧光的药物样分子是生物成像探针的一个有价值的来源。通过在液滴微阵列中进行组合合成和化学文库筛选，我们能够鉴定出新类型的荧光团。通过多组分反应进行简洁而干净的组装，为一步法合成数千种结构多样的荧光分子提供了独特的潜力。由于这些荧光团基于药物样骨架，因此保留了其分子识别潜力，可以用于设计特定的成像探针。
