Beijing National Laboratory for Molecular Sciences (BNLMS), State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry Chinese Academy of Sciences, Beijing, 100190, P. R. China.
University of Chinese Academy of Sciences, Beijing, 100049, P. R. China.
J Mater Chem B. 2022 Jan 19;10(3):430-437. doi: 10.1039/d1tb02296b.
Emerging studies have shown that mitochondrial G-quadruplex plays a critical role in regulating mitochondrial gene replication and transcription, which makes it a promising target for the diagnosis and treatment of cancer or other major diseases. Molecular compounds that can highly target the mitochondrial G-quadruplexes in live cells are essential for further revealing the function and mechanism of these G-quadruplexes. Here, we have developed an organic molecular compound that can highly target the mitochondria of living cells by virtue of the membrane potential mechanism. Then it shows high selectivity to the G-quadruplex structure in the mitochondria, and its fluorescence overlaps well with that of the BG4 antibody. Moreover, the compound has extremely low cytotoxicity and does not interfere with the natural state of G-quadruplex structure. With these good properties, this compound will have great potential in mitochondrial G-quadruplex tracking research or targeted drug screening.
新兴研究表明,线粒体 G-四链体在调节线粒体基因复制和转录中起着关键作用,这使其成为癌症或其他重大疾病诊断和治疗的有前途的靶点。能够在活细胞中高度靶向线粒体 G-四链体的分子化合物对于进一步揭示这些 G-四链体的功能和机制至关重要。在这里,我们开发了一种有机分子化合物,它可以通过膜电位机制高度靶向活细胞的线粒体。然后,它对线粒体中的 G-四链体结构表现出很高的选择性,其荧光与 BG4 抗体的荧光很好地重叠。此外,该化合物具有极低的细胞毒性,并且不干扰 G-四链体结构的自然状态。具有这些良好特性,该化合物将在线粒体 G-四链体跟踪研究或靶向药物筛选方面具有巨大潜力。