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    Structure based design of a novel class of aminopyrimidine MTH1 (MutT homolog 1) inhibitors is described. Optimization led to identification of IACS-4759 (compound 5), a sub-nanomolar inhibitor of MTH1 with excellent cell permeability and good metabolic stability in microsomes. This compound robustly inhibited MTH1 activity in cells and proved to be an excellent tool for interrogation of the utility of MTH1 inhibition in the context of oncology. Copyright © 2016 Elsevier Ltd. All rights reserved.

    Citation

    Alessia Petrocchi, Elisabetta Leo, Naphtali J Reyna, Matthew M Hamilton, Xi Shi, Connor A Parker, Faika Mseeh, Jennifer P Bardenhagen, Paul Leonard, Jason B Cross, Sha Huang, Yongying Jiang, Mario Cardozo, Giulio Draetta, Joseph R Marszalek, Carlo Toniatti, Philip Jones, Richard T Lewis. Identification of potent and selective MTH1 inhibitors. Bioorganic & medicinal chemistry letters. 2016 Mar 15;26(6):1503-7


    PMID: 26898335

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