Department of Chemistry, College of Science, Huazhong Agricultural University, Wuhan 430070, China.
Department of Chemistry, College of Science, Huazhong Agricultural University, Wuhan 430070, China.
Bioorg Med Chem Lett. 2021 May 15;40:127971. doi: 10.1016/j.bmcl.2021.127971. Epub 2021 Mar 19.
The fluorescence probes with high selectivity and sensitivity for telomeric multimeric G-quadruplexes have attracted much attention. Nevertheless, few small molecules have exhibited telomeric multimeric G-quadruplexes recognition specificity. Thus, there is an urgent demand to develop specific fluorescence probes for telomeric multimeric G-quadruplexes. We reported herein the specific sensing of telomeric dimeric G-quadruplex TTA45 via a fluorescence light-up response using a commercially available triazine derivative HPTA-1 as a probe. HPTA-1 could discriminate the telomeric dimeric G-quadruplex TTA45 against other types of DNA structures accompanied by a drastic enhancement of the emission intensity without compromising the conformation and stability. Compared with most multimeric G-quadruplex recognition ligands, HPTA-1 had much simpler structure and lower molecular weight. The binding mechanism studies suggested that the distinct fluorescence response was caused by electrostatic and π-π stacking interactions of HPTA-1 with the pocket between two G-quadruplex units of telomeric dimeric G-quadruplex TTA45..
对端粒多聚 G-四链体具有高选择性和高灵敏度的荧光探针引起了广泛关注。然而，很少有小分子表现出端粒多聚 G-四链体识别特异性。因此，迫切需要开发用于端粒多聚 G-四链体的特异性荧光探针。我们在此报道了使用市售的三嗪衍生物 HPTA-1 作为探针，通过荧光点亮反应对端粒二聚体 G-四链体 TTA45 进行特异性传感。HPTA-1 可以区分端粒二聚体 G-四链体 TTA45 与其他类型的 DNA 结构，同时伴随着发射强度的急剧增强，而不会影响构象和稳定性。与大多数多聚 G-四链体识别配体相比，HPTA-1 具有更简单的结构和更低的分子量。结合机制研究表明，独特的荧光响应是由 HPTA-1 与端粒二聚体 G-四链体 TTA45 两个 G-四链体单元之间口袋的静电和π-π堆积相互作用引起的。
