靶点“钩钓”的光亲和基团的合成及应用进展

    Advances in the Synthesis and Application of Photoaffinity Groups of "Target Fishing"

    • 摘要: 药物分子与靶标的相互作用是其发挥药理活性的基础。靶点“钩钓”作为一种确定靶标的新兴技术,被广泛应用于生物活性成分靶标的识别,但是活性成分与靶标的结合在靶标识别过程中易被破坏,因此,越来越多的光亲和标记探针被开发出来,目的是提高药物分子与靶标结合的稳定性。本文对近年来的光亲和标记探针中的光亲和基团的种类及应用进行综述。

       

      Abstract: The interaction between drug molecule and its target is the basis for its pharmacological activity. "Target fishing", as an emerging technology to identify targets, is widely used in the identification of targets of biologically active ingredients, but there is a problem that the active ingredient is hydrolysed by proteases after binding to the target and is thus unstable, so more and more photo-affinity-labelled probes have been developed with the aim of improving its binding stability. This paper reviewed the types and applications of photoaffinity groups in photoaffinity labelled probes in recent years.

       

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