A new wave of innovations within the DNA damage response

Q Li, W Qian, Y Zhang, L Hu, S Chen… - Signal Transduction and …, 2023 - nature.com
Genome instability has been identified as one of the enabling hallmarks in cancer. DNA
damage response (DDR) network is responsible for maintenance of genome integrity in …

PARP inhibitors for ovarian cancer: current indications, future combinations, and novel assets in development to target DNA damage repair

PA Konstantinopoulos, S Lheureux… - American Society of …, 2020 - ascopubs.org
PARP inhibitors (PARPIs) have revolutionized the treatment of epithelial ovarian cancer, first
for BRCA-associated cancer, and, recently, for all epithelial cancers of serous or high-grade …

Identification of functional pathways and molecular signatures in neuroendocrine neoplasms by multi-omics analysis

V Melone, A Salvati, D Palumbo, G Giurato… - Journal of translational …, 2022 - Springer
Abstract Background Neuroendocrine neoplasms (NENs) represent a heterogeneous class
of rare tumors with increasing incidence. They are characterized by the ability to secrete …

Recurrent glioblastoma: ongoing clinical challenges and future prospects

E Pineda, M Domenech, A Hernández… - OncoTargets and …, 2023 - Taylor & Francis
Virtually all glioblastomas treated in the first-line setting will recur in a short period of time,
and the search for alternative effective treatments has so far been unsuccessful. Various …

Brain exposure of the ATM inhibitor AZD1390 in humans—a positron emission tomography study

A Jucaite, P Stenkrona, Z Cselényi, S De Vita… - Neuro …, 2021 - academic.oup.com
Background The protein kinase ataxia telangiectasia mutated (ATM) mediates cellular
response to DNA damage induced by radiation. ATM inhibition decreases DNA damage …

ATM-SPARK: A GFP phase separation–based activity reporter of ATM

X Li, CI Chung, JJ Yang, S Chaudhuri, PN Munster… - Science …, 2023 - science.org
The kinase ataxia telangiectasia mutated (ATM) plays a key role in the DNA damage
response (DDR). It is thus essential to visualize spatiotemporal dynamics of ATM activity …

Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration

JG Kettle, SK Bagal, D Barratt… - Journal of Medicinal …, 2023 - ACS Publications
The glycine to cysteine mutation at codon 12 of Kirsten rat sarcoma (KRAS) represents an
Achilles heel that has now rendered this important GTPase druggable. Herein, we report our …

Small-molecule targeted therapies induce dependence on DNA double-strand break repair in residual tumor cells

M Ali, M Lu, HX Ang, RS Soderquist, CE Eyler… - Science translational …, 2022 - science.org
Residual cancer cells that survive drug treatments with targeted therapies act as a reservoir
from which eventual resistant disease emerges. Although there is great interest in …

Discovery and evaluation of 3-quinoxalin urea derivatives as potent, selective, and orally available ATM inhibitors combined with chemotherapy for the treatment of …

D Deng, Y Yang, Y Zou, K Liu, C Zhang… - Journal of Medicinal …, 2023 - ACS Publications
ATM plays an important role in DNA damage response and is considered a potential target
in cancer therapies. In this study, a goal-directed molecular generation approach based on …

Targeting ATM and ATR for cancer therapeutics: Inhibitors in clinic

B Priya, S Ravi, S Kirubakaran - Drug Discovery Today, 2023 - Elsevier
Highlights•Genome sequencing has made personalized therapy the preferred cancer
therapeutic approach.•In the past decade, the relevance of targeting DDR kinases for cancer …