State-of-the-art strategies for targeting the DNA damage response in cancer

PG Pilié, C Tang, GB Mills, TA Yap - Nature reviews Clinical oncology, 2019 - nature.com
Genomic instability is a key hallmark of cancer that arises owing to defects in the DNA
damage response (DDR) and/or increased replication stress. These alterations promote the …

Targeting DNA repair in cancer: beyond PARP inhibitors

JS Brown, B O'Carrigan, SP Jackson, TA Yap - Cancer discovery, 2017 - AACR
Germline aberrations in critical DNA-repair and DNA damage–response (DDR) genes
cause cancer predisposition, whereas various tumors harbor somatic mutations causing …

CHK2 kinase in the DNA damage response and beyond

L Zannini, D Delia, G Buscemi - Journal of molecular cell …, 2014 - academic.oup.com
The serine/threonine kinase CHK2 is a key component of the DNA damage response. In
human cells, following genotoxic stress, CHK2 is activated and phosphorylates> 20 proteins …

Targeting the ATR-CHK1 axis in cancer therapy

S Rundle, A Bradbury, Y Drew, NJ Curtin - Cancers, 2017 - mdpi.com
Targeting the DNA damage response (DDR) is a new therapeutic approach in cancer that
shows great promise for tumour selectivity. Key components of the DDR are the ataxia …

Targeting the replication stress response in cancer

JV Forment, MJ O'Connor - Pharmacology & therapeutics, 2018 - Elsevier
Many conventional chemotherapies used in cancer treatment exert their effect by inflicting
DNA damage. Highly proliferative tissues, as well as tumour cells, are particularly vulnerable …

Trial watch: targeting ATM–CHK2 and ATR–CHK1 pathways for anticancer therapy

G Manic, F Obrist, A Sistigu, I Vitale - Molecular & cellular oncology, 2015 - Taylor & Francis
The ataxia telangiectasia mutated serine/threonine kinase (ATM)/checkpoint kinase 2
(CHEK2, best known as CHK2) and the ATM and Rad3-related serine/threonine kinase …

Quantitative structure–activity relationship: promising advances in drug discovery platforms

T Wang, MB Wu, JP Lin, LR Yang - Expert opinion on drug …, 2015 - Taylor & Francis
Introduction: Quantitative structure–activity relationship (QSAR) modeling is one of the most
popular computer-aided tools employed in medicinal chemistry for drug discovery and lead …

Targeting the DNA damage response and DNA repair pathways to enhance radiosensitivity in colorectal cancer

S Deng, T Vlatkovic, M Li, T Zhan, MR Veldwijk… - Cancers, 2022 - mdpi.com
Simple Summary The DNA damage response pathway plays a critical role in maintaining
genomic integrity. Therefore, inhibition of activation of cell-cycle checkpoints involved in this …

ATM, ATR, CHK1, CHK2 and WEE1 inhibitors in cancer and cancer stem cells

C Ronco, AR Martin, L Demange, R Benhida - Medchemcomm, 2017 - pubs.rsc.org
DNA inevitably undergoes a high number of damages throughout the cell cycle. To preserve
the integrity of the genome, cells have developed a complex enzymatic machinery aimed at …

DNA folds threaten genetic stability and can be leveraged for chemotherapy

J Zell, FR Sperti, S Britton, D Monchaud - RSC Chemical Biology, 2021 - pubs.rsc.org
Damaging DNA is a current and efficient strategy to fight against cancer cell proliferation.
Numerous mechanisms exist to counteract DNA damage, collectively referred to as the DNA …