Exploiting replicative stress to treat cancer

M Dobbelstein, CS Sørensen - Nature reviews Drug discovery, 2015 - nature.com
DNA replication in cancer cells is accompanied by stalling and collapse of the replication
fork and signalling in response to DNA damage and/or premature mitosis; these processes …

[HTML][HTML] Deregulation of the EGFR/PI3K/PTEN/Akt/mTORC1 pathway in breast cancer: possibilities for therapeutic intervention

NM Davis, M Sokolosky, K Stadelman, SL Abrams… - Oncotarget, 2014 - ncbi.nlm.nih.gov
Abstract The EGFR/PI3K/PTEN/Akt/mTORC1/GSK-3 pathway plays prominent roles in
malignant transformation, prevention of apoptosis, drug resistance and metastasis. The …

Generating single cell–derived knockout clones in mammalian cells with CRISPR/Cas9

CJ Giuliano, A Lin, V Girish… - Current protocols in …, 2019 - Wiley Online Library
CRISPR/Cas9 technology enables the rapid generation of loss‐of‐function mutations in a
targeted gene in mammalian cells. A single cell harboring those mutations can be used to …

CRISPR/Cas9 mutagenesis invalidates a putative cancer dependency targeted in on-going clinical trials

A Lin, CJ Giuliano, NM Sayles, JM Sheltzer - Elife, 2017 - elifesciences.org
The Maternal Embryonic Leucine Zipper Kinase (MELK) has been reported to be a genetic
dependency in several cancer types. MELK RNAi and small-molecule inhibitors of MELK …

Dual functions of cyclometalated iridium (III) complexes: anti-metastasis and lysosome-damaged photodynamic therapy

FX Wang, MH Chen, YN Lin, H Zhang… - … applied materials & …, 2017 - ACS Publications
Four phosphorescent cyclometalated iridium (III) complexes containing benzimidazole
moiety have been designed and synthesized. These Ir (III) complexes can effectively inhibit …

MELK is not necessary for the proliferation of basal-like breast cancer cells

HT Huang, HS Seo, T Zhang, Y Wang, B Jiang, Q Li… - Elife, 2017 - elifesciences.org
Thorough preclinical target validation is essential for the success of drug discovery efforts. In
this study, we combined chemical and genetic perturbants, including the development of a …

Transforming targeted cancer therapy with PROTACs: A forward-looking perspective

W Farnaby, M Koegl, DB McConnell, A Ciulli - Current opinion in …, 2021 - Elsevier
Small-molecule targeted protein degraders have in recent years made a great impact on the
strategies of many industry and academic cancer research endeavours. We seek here to …

Impact of novel miR-145-3p regulatory networks on survival in patients with castration-resistant prostate cancer

Y Goto, A Kurozumi, T Arai, N Nohata, S Kojima… - British journal of …, 2017 - nature.com
Background: Despite recent advancements, metastatic castration-resistant prostate cancer
(CRPC) is not considered curative. Novel approaches for identification of therapeutic targets …

Maternal embryonic leucine zipper kinase (MELK) as a novel mediator and biomarker of radioresistance in human breast cancer

C Speers, SG Zhao, V Kothari, A Santola, M Liu… - Clinical Cancer …, 2016 - AACR
Purpose: While effective targeted therapies exist for estrogen receptor–positive and HER2-
positive breast cancer, no such effective therapies exist for triple-negative breast cancer …

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 …