β–折叠结构对蛋白质的功能具有重要影响，利用荧光技术研究β–折叠结构与蛋白质（受体）的相互作用具有极大的科学意义和实用价值，它的模拟合成也是多肽化学研究的难点。利用非天然氨基酸形成U型结构模拟β–转角，进而诱导β–折叠的形成是其人工合成最理想的方法，然而在众多β–转角模拟物中，无人采用荧光化合物。本项目首次采用具有优良荧光性质的氟化硼二吡咯（BODIPY）模拟β–折叠结构中的β–转角单元，在此基础上设计、合成多个具有β–折叠结构的生物活性分子，探索其作为荧光探针在生物医药方面的应用前景。主要内容包括：对BODIPY结构进行设计，合成基于BODIPY的荧光β–转角模拟物；以合成somatostatin analogues，多肽P3378-1和ZD2-1为例，通过荧光技术研究其生物活性，探索得到的荧光β–转角模拟物的应用前景；将此技术模板化，推广运用到其它多肽–蛋白、蛋白–蛋白相互作用领域。

As one of the most typical secondary structures, β-sheet has a crucial influence on the function of proteins, using fluorescence techniques to study the interaction between β-sheets and proteins (receptors) has great scientific significance and practical value, the synthesis of protein secondary structure mimics is also the difficulty in peptide chemistry. Using unnatural amino acids as templates to induce β-sheet structure in small peptides is most advantageous, because these templates eliminated most of the entropic penalty associated with chain reversal due to their U shape, however, to the best of our knowledge, none of these compounds have been reported to be fluorescent. This project is firstly proposed using 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) as research object for the development of fluorescent β-turn mimics, since it not only would lead to short conformationally restricted peptides, but also could be easily detected and studied by fluorescence techniques. On this basis, designing and synthesizing different bioactive β-sheet mimics to explore their biomedical applications as fluorescent probes. The concrete content includes: Design and synthesis of fluorescent β-turn mimics based on BODIPY; Synthesizing somatostatin analogues, peptide P3378-1 and ZD2-1 as examples to explore the application prospect of fluorescent β-turn mimics, the binding ability of fluorescent peptides to their receptors were studied by fluorescence anisotropy and their abilities as a fluorescent probe for detecting tumor cells were investigated by fluorescence imaging technology; Finally, generalize this technology to research other field of peptide-protein, protein-protein interactions for providing useful information in designing potential drug candidates.