Oak Brook, IL – Volume 34 of SLAS Discovery includes two original research articles, one short communication and one entry in the upcoming Special Issue on EUOS/SLAS Joint Challenge: Compound Solubility.
Original Research
- Development of a high-throughput TR-FRET assay to identify inhibitors of the FAK-paxillin protein-protein interaction
This study presents a high-throughput TR-FRET assay targeting the FAK FAT domain's interaction with paxillin, identifying four novel small-molecule inhibitors with potential applications in cancer and fibrosis therapy. The screening strategy combined TR-FRET primary/counterscreen assays and SPR validation to ensure specificity, establishing a robust framework for future FAK PPI drug discovery.
- Parallel in vitro ion channel and in vivo zebrafish assaying of elapid snake venoms following chromatographic separation of toxin components
This article introduces an integrated high-throughput platform combining nanofractionation analytics, calcium flux assays, zebrafish paralysis tests and proteomics to rapidly identify and characterize snake venom toxins targeting ion channels, demonstrating its utility with elapid venoms.
Short Communication
- Optimization and development of a high-throughput TR-FRET screening assay for SLIT2/ROBO1 interaction
The authors demonstrate a high-throughput TR-FRET assay for screening inhibitors of the oncogenic SLIT2/ROBO1 interaction, identifying SMIFH2 as a dose-dependent disruptor. This discovery provides the first pharmacological tool to target this pathway in cancer, fibrosis and vascular diseases.
Special Issue
The upcoming special issue, EUOS/SLAS Joint Challenge: Compound Solubility highlights a scientific challenge in which computational experts developed machine learning models to predict solubility for ~100,000 compounds from the EU-OPENSCREEN collection. The challenge prioritized interpretable AI workflows, combining robust data curation with meaningful chemical descriptors to create a benchmark for future solubility prediction in drug discovery.
Access to this issue of SLAS Discovery is available at https://www.slas-discovery.org/issue/S2472-5552(25)X0005-8
