A "three-in-one" multi-functional probe for Bcl-2/Mcl-1 profiling and visualizing in situ

Xiaodong Zhang, Ziqian Wang, Zongwei Guo, Ting Song, Nianzhe He, Junjie Zhu, Keke Cao, Zhichao Zhang*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

Bcl-2 and Mcl-1, the two arms of the anti-apoptotic Bcl-2 family proteins, have been identified as key regulators of apoptosis and effective therapeutic targets of cancer. However, no small molecular probe is capable of profiling and visualizing both Bcl-2 and Mcl-1 simultaneously in situ . Herein, we reported a multi-functional molecular probe ( BnN 3 -OPD-Alk ) by a "three-in-one" molecular designing strategy, which integrated the Bcl-2/Mcl-1 binding ligand, fluorescent reporter group and photoreactive group azido into the same scaffold. BnN 3 -OPD-Alk exhibited sub-μM affinities to Bcl-2/Mcl-1 and bright green self-fluorescence. It was then successfully applied for Bcl-2/Mcl-1 labelling, capturing, enriching, and bioimaging both in vitro and in cells. This strategy could facilitate the precise early diagnosis and effective therapy of dual Bcl-2/Mcl-1-related diseases.

Original languageEnglish
JournalChemBioChem
Volume22
Issue number2
Pages (from-to)326-329
ISSN1439-4227
DOIs
Publication statusPublished - 2021

Bibliographical note

© 2020 Wiley-VCH GmbH.

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