142246-48-8Relevant articles and documents
Environment-sensitive fluorescent inhibitors of histone deacetylase
Dong, Gaopan,Du, Lupei,Li, Minyong,Li, Zhenzhen,Qin, Xiaojun,Song, Tianjia,Wang, Guankai,Zhou, Xin
, (2020)
Histone deacetylases (HDACs) are proteases that can catalyze the deacetylation of histones to inhibit gene transcription. Since mutations and/or aberrant expression of various HDACs are frequently associated with human diseases, particularly cancers, HDACs are important therapeutic targets for many human tumors. However, there are still relatively few studies on HDAC small molecule fluorescent probes. Herein, we designed and synthesized a class of environment-sensitive fluorescent inhibitors with a switch mechanism to study HDAC activity. In vitro, the enzyme inhibition activity of compound 6b was comparable to the positive control drug SAHA, and it presented suitable imaging in living cells and tumor-tissue slices. This environment-sensitive fluorescent inhibitor provides a new idea for the diagnosis and treatment of HDACs-related diseases.
Environment-sensitive turn-on fluorescent probes for p53-MDM2 protein-protein interaction
Liu, Tingting,Jiang, Yan,Liu, Zhenzhen,Li, Jin,Fang, Kun,Zhuang, Chunlin,Du, Lupei,Fang, Hao,Sheng, Chunquan,Li, Minyong
, p. 1668 - 1672 (2017)
A series of probes with a turn-on switch for the p53-MDM2 protein-protein interaction were developed. After careful evaluation, these small molecule fluorescent probes exhibited high practical activity and selectivity in vitro and in cellulo. In particular probe 10, which had a Ki value of 0.03 μM, displayed much better binding affinity compared to the positive control Nutlin-3, which had a Ki value of 0.23 μM. These no-wash environment-sensitive turn-on fluorescent probes have been successfully applied to imaging p53-MDM2 interaction in the human lung cancer cell line A549 (wild-type p53) at the micromolar level. Therefore, these fluorescent probes are expected to be used in drug screening and cell staining in p53-MDM2 fields, as well as in pathological and physiological studies of the p53-MDM2 interaction.
Investigation of thiolysis of 4-substituted SBD derivatives and rational design of a GSH-selective fluorescent probe
Ji, Xiuru,Li, Shan,Sun, Lu,Tu, Xiaoqiang,Xi, Zhen,Yang, Chao,Ye, Haishun,Yi, Long
, p. 6527 - 6533 (2021)
In order to evaluate 7-sulfonamide benzoxadiazole (SBD) derivatives for the development of fluorescent probes, herein we investigated the thiolysis reactivity and selectivity of a series of SBD compounds with different atoms (N/O/S/Se) at the 4-position.
