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2020 1
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Page 1
Selective Inhibition of ATM-dependent Double-strand Break Repair and Checkpoint Control Synergistically Enhances the Efficacy of ATR Inhibitors.
Turchick A, Zimmermann A, Chiu LY, Dahmen H, Elenbaas B, Zenke FT, Blaukat A, Vassilev LT. Turchick A, et al. Mol Cancer Ther. 2023 Jul 5;22(7):859-872. doi: 10.1158/1535-7163.MCT-22-0685. Mol Cancer Ther. 2023. PMID: 37079339 Free PMC article.
In cancer cells with functional ATM and p53 signaling, selective suppression of ATR catalytic activity by M6620 induced G1-phase arrest to prevent S-phase entry with unrepaired DSBs. The selective ATM inhibitors, M3541 and M4076, suppressed both ATM-dependent cell-cycle ch …
In cancer cells with functional ATM and p53 signaling, selective suppression of ATR catalytic activity by M6620 induced G1-phase arrest to p …
Selective ATM inhibition augments radiation-induced inflammatory signaling and cancer cell death.
Chiu LY, Sun Q, Zenke FT, Blaukat A, Vassilev LT. Chiu LY, et al. Aging (Albany NY). 2023 Jan 17;15(2):492-512. doi: 10.18632/aging.204487. Epub 2023 Jan 17. Aging (Albany NY). 2023. PMID: 36656721 Free PMC article.
We recently reported two new potent and selective ATM inhibitors, M3541 and M4076, that effectively sensitize cancer cells to radiation and regress human xenografts in clinically relevant animal models. ...
We recently reported two new potent and selective ATM inhibitors, M3541 and M4076, that effectively sensitize cancer cells to radiati …
A New Class of Selective ATM Inhibitors as Combination Partners of DNA Double-Strand Break Inducing Cancer Therapies.
Zimmermann A, Zenke FT, Chiu LY, Dahmen H, Pehl U, Fuchss T, Grombacher T, Blume B, Vassilev LT, Blaukat A. Zimmermann A, et al. Mol Cancer Ther. 2022 Jun 1;21(6):859-870. doi: 10.1158/1535-7163.MCT-21-0934. Mol Cancer Ther. 2022. PMID: 35405736 Free PMC article.
Here, we describe the pharmacological activities of two highly potent and selective ATM inhibitors from a new chemical class, M3541 and M4076. In biochemical assays, they inhibited ATM kinase activity with a sub-nanomolar potency and showed remarkable selectivity against o …
Here, we describe the pharmacological activities of two highly potent and selective ATM inhibitors from a new chemical class, M3541 and M …
Molecular basis of human ATM kinase inhibition.
Stakyte K, Rotheneder M, Lammens K, Bartho JD, Grädler U, Fuchß T, Pehl U, Alt A, van de Logt E, Hopfner KP. Stakyte K, et al. Nat Struct Mol Biol. 2021 Oct;28(10):789-798. doi: 10.1038/s41594-021-00654-x. Epub 2021 Sep 23. Nat Struct Mol Biol. 2021. PMID: 34556870
We determined the structure of the kinase domain bound to ATPgammaS and to the ATM inhibitors KU-55933 and M4076 at 2.8 A, 2.8 A and 3.0 A resolution, respectively. The mode of action and selectivity of the ATM inhibitors can be explained by structural comparison and provi …
We determined the structure of the kinase domain bound to ATPgammaS and to the ATM inhibitors KU-55933 and M4076 at 2.8 A, 2.8 A and …
Gender diversity in academic medicine.
Stewart-Brown S. Stewart-Brown S. BMJ. 2020 Oct 26;371:m4076. doi: 10.1136/bmj.m4076. BMJ. 2020. PMID: 33106233 No abstract available.