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Showing 1–7 of 7 results
Advanced filters: Author: Matthieu Desroses Clear advanced filters

  • TH1760 is a first-in-class, potent, selective and cell-active inhibitor against human NUDT15, which sensitizes cells to 6-thioguanine treatment. TH1760 represents a valuable tool for deciphering the enigmatic functions of NUDT15.

    • Si Min Zhang
    • Matthieu Desroses
    • Thomas Helleday
    Research
    Nature Chemical Biology
    Volume: 16, P: 1120-1128

  • Cellular target engagement technologies enable quantification of intracellular drug binding, but the simultaneous assessment of drug-associated phenotypes is challenging. Here, the authors develop CeTEAM (cellular target engagement by accumulation of mutant), a platform that can simultaneously evaluate drug-target interactions and phenotypic responses for holistic assessment of drug pharmacology using conditionally stabilized drug biosensors.

    • Nicholas C. K. Valerie
    • Kumar Sanjiv
    • Mikael Altun
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-22

  • Dysfunctional redox regulation in cancer can damage dNTPs so inhibiting dNTP pool sanitizing enzymes, such as MTH1, is a potential cancer treatment. Here, Carter et al.characterize MTH2 (NUDT15) and show that it is not a dNTP sanitizer, and so is unlikely to influence the efficacy of MTH1 inhibitors.

    • Megan Carter
    • Ann-Sofie Jemth
    • Pål Stenmark
    ResearchOpen Access
    Nature Communications
    Volume: 6, P: 1-10

  • Several tuberculosis drugs are prodrugs that have to be enzymatically activated during metabolism. Ethionamide is such a drug and is activated by the monooxygenase EthA. EthA is itself regulated by the transcriptional repressor EthR. Here Alain Baulard and his colleagues have designed inhibitors of EthR that boost the antimycobacterial efficacy of ethionamide both in vitro and in vivo. Current therapy with ethionamide requires the use of high doses, often eliciting side effects. Its combination with the EthR repressor should allow lower doses to be used.

    • Nicolas Willand
    • Bertrand Dirié
    • Alain R Baulard
    Research
    Nature Medicine
    Volume: 15, P: 537-544

  • In order to find a general treatment for cancer, this study found that MTH1 activity is essential for the survival of transformed cells, and isolated two small-molecule inhibitors of MTH1, TH287 and TH588 — in the presence of these inhibitors, damaged nucleotides are incorporated into DNA only in cancer cells, causing cytotoxicity and eliciting a beneficial response in patient-derived mouse xenograft models.

    • Helge Gad
    • Tobias Koolmeister
    • Thomas Helleday
    Research
    Nature
    Volume: 508, P: 215-221