Scientists have discovered a new drug which may inhibit the growth of cancer cells by zeroing in on mutated nuclear receptors that promote tumours. The anti-cancer agent could have broad therapeutic applications as it prevents activation of the PI3K pathway, which is common to many cancers. "K-80003 binds specifically to a truncated form of the retinoid X receptor-alpha (tRXRa) protein that promotes tumours," said a professor at Sanford Burnham Prebys Medical Discovery Institute (SBP) in the US."When it binds tRXRa, it freezes the protein into an inactive (tetrameric) configuration that prevents it from stimulating the PI3K pathway," he said.
"We wanted to visualise how tRXRa and K-80003 physically interact - at atomic resolution - in a way that makes this such a promising cancer drug," he said. "We know tRXRa protein is specifically produced by tumour cells, while normal cells only…
