Drug Discovery Laboratory (Norway)

Modification Technology for Exosome Membranes using Membrane-Curvature-Sensing Peptides and Its Application to Boron Neutron Capture Therapy

Abstract Extracellular vesicles such as exosomes are expected to be used as drug delivery vehicles, particularly in personalized medicine, due to their pharmacological advantages. However, the development of functionalization techniques for isolated extracellular vesicles—includi...

Hsc70-Mediated Targeting Chimeras for Targeted Protein Degradation via Chaperone-Mediated Autophagy

Abstract Despite the remarkable success of proteolysis-targeting chimeras (PROTACs), challenges such as limited applicability to certain cytosolic proteins, potential resistance risks, and off-target effects remain. Novel degradation strategies harnessing the autophagy/lysosome p...

UA-30 ameliorates motor deficits through RalA-mediated mitophagy in ALS mice

Amyotrophic lateral sclerosis (ALS) is a neurodegenerative disease characterized by progressive motor neuron loss, skeletal muscle atrophy, paralysis, and eventually death. Mitochondrial dysfunction plays a pivotal role in ALS pathogenesis, although the precise pathogenic mechani...

A selectivity-aware machine-learning workflow for prioritizing CDK2-biased kinase inhibitor candidates

Abstract Cyclin-dependent kinase 2 (CDK2) is a therapeutic target of interest, but selective inhibition remains challenging because ATP-competitive inhibitors often engage related CDK family members. Here, we developed a selectivity-aware computational workflow to prioritize CDK2...

Dual plasmepsin IX and X inhibitors are refractory to development of resistance

Abstract Artemisinin-based combination therapies (ACTs) remain the cornerstone of malaria treatment, but emerging resistance threatens their efficacy. The potential for the development of drug resistance against plasmepsin X (PMX)-selective inhibitors and dual plasmepsin IX/X (PM...

Robust out-of-distribution prediction of Buchwald–Hartwig reactions

Abstract The Buchwald–Hartwig cross-coupling is a cornerstone of modern pharmaceutical synthesis, yet predictive modeling of its outcomes remains constrained by data quality and chemical space coverage. Electronic laboratory notebooks contain heterogeneous, noisy records, while o...