Oak Brook, IL – Volume 33 of SLAS Discovery features one review, three original research articles and one entry in the upcoming Special Issue on Biomolecular Condensates as Targets for Drug Discovery.
Reviews
- Antimicrobial resistance: Linking molecular mechanisms to public health impact
This review highlights how β-lactamases and efflux pumps, combined with mobile genetic elements, drive the rapid spread of multidrug-resistant (MDR) and extremely drug-resistant (XDR) pathogens, posing a serious threat to global health and agriculture.
Original Research
- Advancing the development of TRIP13 inhibitors: A high-throughput screening approach
In this study, the researchers developed a high-throughput luminescence-based assay to screen for TRIP13 inhibitors, identifying anlotinib as a promising candidate. Their discovery presents a new approach for targeting TRIP13 in cancers that are resistant to therapy and deficient in retinoblastoma.
- Combinatorial screen with apoptosis pathway targeted agents alrizomadlin, pelcitoclax, and dasminapant in multi-cell type tumor spheroids
This research assesses the effectiveness of apoptosis-targeting drugs—alrizomadlin, pelcitoclax and dasminapant—in solid tumor spheroids, both alone and in combination with other therapies. The results emphasize the potential of modifying the apoptosis pathway to improve cancer treatment in various aggressive solid tumors.
- The authors identify small-molecule inhibitors of hyperphosphorylated tau aggregation and neurotoxicity through a high-throughput screen, offering a promising new therapeutic strategy for Alzheimer's disease and related tauopathies by directly targeting tau pathology.
Biomolecular Condensates as Targets for Drug Discovery
This upcoming Special Issue, guest edited by Charles P. Hart, PhD (University of California, San Francisco), will explore the role of biomolecular condensates in diseases and the potential for drug discovery by modulating their formation, stability or dissolution in neurodegenerative, cancer and inflammatory disorders.
- A biochemical screening platform to target chromatin states using condensates as a tool
This study presents a novel drug discovery approach that targets dysfunctional chromatin states by leveraging their phase-separated condensate properties, enabling the identification of context-specific small-molecule modulators to reduce off-target effects and enhance therapeutic potential.
Access to this issue of SLAS Discovery is available at https://www.slas-discovery.org/issue/S2472-5552(25)X0004-6
