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Arsenic trioxide targets Hsp60, triggering degradation of p53 and survivin

Xuqiao Hu, Hongyan Li, Tiffany Ka-Yan Ip, Hilaire Yam Fung Cheung, Mohamad Koohi‐Moghadam, Haibo Wang, Xinming Yang, Daniel N. Tritton, Yuchuan Wang, Yi Wang, Runming Wang, Kwan‐Ming Ng, Hua Naranmandura, Eric Tse, Hongzhe Sun

2021Chemical Science44 citationsDOIOpen Access PDF

Abstract

) with quantitative proteomics, allowing 37 arsenic binding and 250 arsenic regulated proteins to be identified in NB4, a human APL cell line. Bioinformatics analysis reveals that ATO disrupts multiple physiological processes, in particular, chaperone-related protein folding and cellular response to stress. Furthermore, we discover heat shock protein 60 (Hsp60) as a vital target of ATO. Through biophysical and cell-based assays, we demonstrate that ATO binds to Hsp60, leading to abolishment of Hsp60 refolding capability. Significantly, the binding of ATO to Hsp60 disrupts the formation of Hsp60-p53 and Hsp60-survivin complexes, resulting in degradation of p53 and survivin. This study provides significant insights into the mechanism of action of ATO at a systemic perspective, and serves as guidance for the rational design of metal-based anticancer drugs.

Topics & Concepts

Arsenic trioxideSurvivinChemistryDegradation (telecommunications)HSP60LeukemiaCancer researchArsenicBiochemistryBiologyComputer scienceHeat shock proteinImmunologyApoptosisHsp70Organic chemistryGeneTelecommunicationsRetinoids in leukemia and cellular processesComputational Drug Discovery MethodsHeat shock proteins research