MutT Homolog 1 (MTH1): The Silencing of a Target

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• 作者：Gianluca Papeo
• 刊名：Journal of Medicinal Chemistry
• 出版年：2016
• 出版时间：March 24, 2016
• 年：2016
• 卷：59
• 期：6
• 页码：2343-2345
• 全文大小：199K
• ISSN：1520-4804

文摘

MTH1 is a member of the nudix phosphohydrolase superfamily of enzymes, and it is involved in nucleotide pool homeostasis. The protein exerts its scavenging action by hydrolyzing oxidized nucleotides, thus avoiding their misincorporation into replicating DNA. Recent reports have validated its inhibition as a potential broad-spectrum target in oncology and have described small molecules able to engage this target with antiproliferative effect. In the accompanying paper (DOI: g/10.1021/acs.jmedchem.5b01760">10.1021/acs.jmedchem.5b01760), a team at AstraZeneca led by Jason G. Kettle elegantly demonstrated the complete lack of antiproliferative activity of cancer cells to highly potent MTH1 inhibitors.