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A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth.

Lei Wang; Jianjun Chang; Diana Varghese; Michael Dellinger; Subodh Kumar; Anne M Best; Julio Ruiz; Richard Bruick; Samuel Peña-Llopis; Junjie Xu; et al.

(Profiled Authors: Rolf A Brekken; Richard K Bruick; Elisabeth D Martinez; Samuel Pena-Llopis; Michael T Dellinger)

Nature communications. 2013;4.

Abstract

The pharmacological inhibition of general transcriptional regulators has the potential to block growth through targeting multiple tumorigenic signalling pathways simultaneously. Here, using an innovative cell-based screen, we identify a structurally unique small molecule (named JIB-04) that specifically inhibits the activity of the Jumonji family of histone demethylases in vitro, in cancer cells, and in tumours in vivo. Unlike known inhibitors, JIB-04 is not a competitive inhibitor of α-ketoglutarate. In cancer, but not in patient-matched normal cells, JIB-04 alters a subset of transcriptional pathways and blocks viability. In mice, JIB-04 reduces tumour burden and prolongs survival. Importantly, we find that patients with breast tumours that overexpress Jumonji demethylases have significantly lower survival. Thus, JIB-04, a novel inhibitor of Jumonji demethylases in vitro and in vivo, constitutes a unique potential therapeutic and research tool against cancer, and validates the use of unbiased cellular screens to discover chemical modulators with disease relevance.


PMID: 23792809    

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