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Anticancer drug discovery: A family of enzymes

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When doctors hurl toxic death at cancer cells, often a few will survive and come back. A family of enzymes called KDM5 histone demethylases is emerging as important for this resilience and drugs that inhibit KDM5 enzymes could be active in treating several types of cancer. A team of investigators obtained detailed structural information, showing how inhibitors of the KDM5 family interact with their targets by building a molecular model of the KDM5A enzyme, along with an inhibitor bound in the active site.

Their findings could inform efforts to design more potent and selective anticancer drugs.

Image credit: From Horton et al, Cell Chem Bio (2016)

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