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A Small Molecule Inauhzin Inhibits SIRT1 Activity and Suppresses Tumour Growth Through Activation of p53

A Small Molecule Inauhzin Inhibits SIRT1 Activity and Suppresses Tumour Growth Through Activation of p53

Qi Zhang, Shelya X Zeng, Yu Zhang, Yiwei Zhang, Derong Ding, Qizhuang Ye, Samy O Meroueh, Hua Lu

EMBO Mol Med. 2012 Apr;4(4):298-312.

PMID: 22331558

Abstract:

Although ∼50% of all types of human cancers harbour wild-type TP53, this p53 tumour suppressor is often deactivated through a concerted action by its abnormally elevated suppressors, MDM2, MDMX or SIRT1. Here, we report a novel small molecule Inauhzin (INZ) that effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress. Moreover, INZ stabilizes p53 by increasing p53 acetylation and preventing MDM2-mediated ubiquitylation of p53 in cells, though not directly in vitro. Remarkably, INZ inhibits cell proliferation, induces senescence and tumour-specific apoptosis, and represses the growth of xenograft tumours derived from p53-harbouring H460 and HCT116 cells without causing apparent toxicity to normal tissues and the tumour-bearing SCID mice. Hence, our study unearths INZ as a novel anti-cancer therapeutic candidate that inhibits SIRT1 activity and activates p53.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP309271941	Inauhzin		309271-94-1	Price

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