Validation and development of MTH1 inhibitors for treatment of cancer.

U Warpman Berglund,K Sanjiv,H Gad,C Kalderén, T Koolmeister,T Pham, C Gokturk,R Jafari,G Maddalo,B Seashore-Ludlow,A Chernobrovkin, A Manoilov,I S Pateras, A Rasti, A-S Jemth, I Almlöf,O Loseva,T Visnes,B O Einarsdottir, F Z Gaugaz,A Saleh, B Platzack,O A Wallner,K S A Vallin, M Henriksson,P Wakchaure,S Borhade,P Herr, Y Kallberg,P Baranczewski,E J Homan, E Wiita, V Nagpal, T Meijer,N Schipper,S G Rudd, L Bräutigam, A Lindqvist,A Filppula,T-C Lee, P Artursson,J A Nilsson,V G Gorgoulis,J Lehtiö,R A Zubarev,M Scobie,T Helleday

Annals of Oncology（2016）

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摘要

Different MTH1 inhibitors have different ability to kill cancer cells. Here we demonstrate that the lack of efficiency of some MTH1 inhibitors is explained by their inability introduce the toxic oxidized nucleotides into DNA. Furthermore, we describe TH1579, Karonudib, which is a potent, selective MTH1 inhibitor with good oral availability and with excellent anti-cancer properties in vivo.

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关键词

MTH1,reactive oxygen species,cancer,small molecule inhibitors,DNA damage

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