Environment-sensitive turn-on fluorescent probes for p53–MDM2 protein–protein interaction,RSC Medicinal Chemistry

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Environment-sensitive turn-on fluorescent probes for p53–MDM2 protein–protein interaction
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-07-03 00:00:00 , DOI: 10.1039/c7md00287d
Tingting Liu _{1,

2,

3,

4,

5} , Yan Jiang _{1,

3,

6,

7,

8} , Zhenzhen Liu _{1,

2,

3,

4,

5} , Jin Li _{1,

3,

6,

7,

8} , Kun Fang _{1,

3,

6,

7,

8} , Chunlin Zhuang _{1,

3,

6,

7,

8} , Lupei Du _{1,

2,

3,

4,

5} , Hao Fang _{1,

2,

3,

4,

5} , Chunquan Sheng _{1,

3,

6,

7,

8} , Minyong Li _{1,

2,

3,

4,

5}

Affiliation

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 K_i value of 0.03 μM, displayed much better binding affinity compared to the positive control Nutlin-3, which had a K_i 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.

中文翻译：

用于p53–MDM2蛋白与蛋白相互作用的环境敏感型开启式荧光探针

开发了一系列带有p53–MDM2蛋白质–蛋白质相互作用的开启开关的探针。经过仔细评估，这些小分子荧光探针在体外和纤维素中均显示出很高的实用活性和选择性。在特定的探针10，它有一个ķ_我0.03μM的值，相对于阳性对照Nutlin-3，它有一个显示更好的结合亲和力ķ_我值为0.23μM。这些无需清洗的环境敏感型开启荧光探针已成功应用于微摩尔水平的人类肺癌细胞系A549（野生型p53）中p53–MDM2相互作用的成像。因此，这些荧光探针有望用于p53–MDM2领域的药物筛选和细胞染色，以及p53–MDM2相互作用的病理和生理研究。

更新日期：2017-08-16

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