ATF4‐mediated stress response as a therapeutic vulnerability in chordoma
We screened 5 chordoma cell lines against 100+ inhibitors of epigenetic and metabolic pathways and kinases and identified halofuginone, a tRNA synthetase inhibitor. Mechanistically halofuginone induces an integrated stress response, with eIF2alpha phosphorylation, activation of ATF4 and its target genes CHOP, ASNS, INHBE leading to cell death ...
Lucia Cottone +11 more
wiley +1 more source
Reproduction of the human relevant potency threshold (HRPT) for estrogen receptor alpha agonism in an inference performance screen for ICCVAM's regulatory scientific confidence framework. [PDF]
Ryman J, Becker RA.
europepmc +1 more source
A subset of MMR‐proficient colon cancers responds to neoadjuvant immunotherapy
Tan et al. reveal that a distinct subset of early‐stage pMMR colon cancers can respond to neoadjuvant immunotherapy. In the NICHE‐2 trial, responders (26%) were characterized by chromosomal instability, TP53 mutations, and proliferative cell‐cycle programs, whereas nonresponders showed metabolic and stromal reprogramming with TGF‐β‐driven ...
Eleonora Piumatti +3 more
wiley +1 more source
Fingerprint-Based Machine Learning for SARS-CoV-2 and MERS-CoV <i>M</i><sup><i>pro</i></sup> Inhibition: Highlighting the Potential of Bayesian Neural Networks. [PDF]
Doering NP +3 more
europepmc +1 more source
The cancer problem is increasing globally with projections up to the year 2050 showing unfavourable outcomes in terms of incidence and cancer‐related deaths. The main challenges are prevention, improved therapeutics resulting in increased cure rates and enhanced health‐related quality of life.
Ulrik Ringborg +43 more
wiley +1 more source
Synthesis and Pharmacological Characterization of Nociceptin/Orphanin FQ Dimeric Ligands. [PDF]
Albanese V +16 more
europepmc +1 more source
LDAcoop: Integrating non‐linear population dynamics into the analysis of clonogenic growth in vitro
Limiting dilution assays (LDAs) quantify clonogenic growth by seeding serial dilutions of cells and scoring wells for colony formation. The fraction of negative wells is plotted against cells seeded and analyzed using the non‐linear modeling of LDAcoop.
Nikko Brix +13 more
wiley +1 more source
Synthetic strategies towards benzothiazole-based compounds of therapeutic potency: experimental, investigational and approved drugs. [PDF]
Mohamed-Ezzat RA, Elgemeie GH.
europepmc +1 more source
Antiviral Potency of Antipsychotics: A New Therapeutic Strength
Hala M. Zeidan, Suheir Amer
openalex +1 more source
Plecstatin inhibits hepatocellular carcinoma tumorigenesis and invasion through cytolinker plectin
The ruthenium‐based metallodrug plecstatin exerts its anticancer effect in hepatocellular carcinoma (HCC) primarily through selective targeting of plectin. By disrupting plectin‐mediated cytoskeletal organization, plecstatin inhibits anchorage‐dependent growth, cell polarization, and tumor cell dissemination.
Zuzana Outla +10 more
wiley +1 more source

