Novel Epigenetic Strategy Provides Cancer Drug Discovery Breakthrough

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Researchers unveil a first-in-class inhibitor that shuts down a key epigenetic switch driving lung cancer growth.

A research team by Professor Xiang David Li from the Department of Chemistry at The University of Hong Kong (HKU), in collaboration with researchers from the Shenzhen Bay Laboratory and Tsinghua University, has made a breakthrough in epigenetic drug discovery. The team has successfully developed a first-in-class chemical inhibitor that precisely and selectively targets the ATAC complex, a critical cellular “switch operator” that activates tumour-promoting genes, opening a novel therapeutic avenue for non-small cell lung cancer (NSCLC). The findings were recently published in the top-tier journal Nature Chemical Biology, and multiple international patent applications have been filed.

Histone Modifications as Genetic Switches in Our Cells

Inside human cells, DNA is wrapped around protein structures called histones to form chromatin. Chemical modifications on histones function like genetic “switches”, determining whether genes are turned on or remain silent.  Among these modifications, histone acetylation is one of the most important “on” switches that activate gene expression. This modification is catalysed by enzyme complexes known as histone acetyltransferases (HATs).


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