Issue 8, 2017

Environment-sensitive turn-on fluorescent probes for p53–MDM2 protein–protein interaction

Abstract

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.

Graphical abstract: Environment-sensitive turn-on fluorescent probes for p53–MDM2 protein–protein interaction

Associated articles

Supplementary files

Article information

Article type
Research Article
Submitted
02 Jun 2017
Accepted
30 Jun 2017
First published
03 Jul 2017

Med. Chem. Commun., 2017,8, 1668-1672

Environment-sensitive turn-on fluorescent probes for p53–MDM2 protein–protein interaction

T. Liu, Y. Jiang, Z. Liu, J. Li, K. Fang, C. Zhuang, L. Du, H. Fang, C. Sheng and M. Li, Med. Chem. Commun., 2017, 8, 1668 DOI: 10.1039/C7MD00287D

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