A New Class of Selective ATM Inhibitors as Combination Partners …
2022年6月1日 · Here, we describe the pharmacological activities of two highly potent and selective ATM inhibitors from a new chemical class, M3541 and M4076. In biochemical …
Molecular basis of human ATM kinase inhibition - Nature
2021年9月23日 · High-resolution cryo-EM structures of human ATM bound to ATPγS and two distinct ATM inhibitors provide insights into the mechanism of inhibitor selectivity and offer a …
Pharmacology of the ATM Inhibitor AZD0156: Potentiation of …
2020年1月3日 · AZD0156 is a potent and selective, bioavailable inhibitor of ataxia-telangiectasia mutated (ATM) protein, a signaling kinase involved in the DNA damage response. We present …
Clinical potential of ATM inhibitors - ScienceDirect
2020年5月1日 · Here, we provide some background on ATM and its activation and investigate the efficacy of ATM inhibitors in treating cancer. 1. Introduction. Savitsky et al. [1] first identified …
Molecular basis of human ATM kinase inhibition - PubMed
Human checkpoint kinase ataxia telangiectasia-mutated (ATM) plays a key role in initiation of the DNA damage response following DNA double-strand breaks. ATM inhibition is a promising …
Small Molecular Inhibitors That Target ATM for Drug Discovery: …
2024年8月16日 · The protein kinase ataxia telangiectasia mutated (ATM) is a constituent of the phosphatidylinositol 3-kinase-related kinase (PIKK) family, exerting a pivotal influence on …
ATM in DNA repair in cancer - PubMed
2020年11月12日 · ATM inhibitors, including KU-55933, KU-60019, KU-59403, CP-466722, AZ31, AZ32, AZD0156, and AZD1390, have been evaluated for their antitumor effects. It has been …
ATM, ATR, CHK1, CHK2 and WEE1 inhibitors in cancer and cancer …
Five kinases play pivotal roles in the DDR: ATM, ATR, CHK1, CHK2 and WEE1. Herein, we review the drugs targeting these proteins and the inhibitors used in the specific case of CSC.
Recent advances in ATM inhibitors as potential therapeutic agents
The mechanism of ATM in cancer treatment and the development of its inhibitors have become research hotspots. Here we present an overview of research concerning ATM protein …
Selective Inhibition of ATM-dependent Double-strand Break …
Using two new ATM inhibitors (M3541 and M4076) and engineered p53-null and ATM-null isogenic clones of the p53/ATM wild-type A549 cells as molecular tools, we interrogated the …