Paul E. Brennan

Discovery of a molecular glue inhibitor that stabilises a non-productive Kalirin-Rac1 complex

The paper identifies covalent molecular glue inhibitors that stabilize a non-productive Kalirin-Rac1 complex, inhibiting nucleotide exchange and reducing GEF turnover.

mBACS enhances pseudouridine profiling through efficient and robust chemical conversion

mBACS improves pseudouridine profiling with higher conversion efficiency and lower false positives, revealing new sites and functional insights into tRNA modifications.

The KDM6 histone demethylase inhibitor GSK-J4 induces metal and stress responses in multiple myeloma cells

This study shows GSK-J4, a KDM6 inhibitor, induces metal and stress responses in multiple myeloma cells by increasing intracellular Zn2+ and activating metallothionein gene expression.

Inhibition of MLLT1 limits growth of MLL-AF4 leukaemias without killing healthy haematopoietic stem cells

This study shows that inhibiting MLLT1 selectively limits MLL-AF4-driven leukemia growth without harming healthy hematopoietic stem cells.

Structural Dynamics of the Ubiquitin Specific Protease USP30 in Complex with a Cyanopyrrolidine-Containing Covalent Inhibitor

This study investigates the structural dynamics of USP30 inhibition by a covalent inhibitor, revealing its binding mechanism and selectivity advantages over non-covalent inhibitors.

Luminescence-based complementation assay to assess target engagement and cell permeability of glycolate oxidase (HAO1) inhibitors.

This paper introduces a luminescence-based CETSA method to measure HAO1 inhibitor uptake and engagement, showing it can differentiate ligand permeability and engagement profiles.

Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM

The paper identifies two covalent inhibitors that disrupt the interaction between SYK's tandem SH2 domains and FCER1G phospho-ITAM, potentially beneficial for Alzheimer's disease therapy.

Development of FERM domain protein-protein interaction inhibitors for MSN and CD44 as a potential therapeutic strategy for Alzheimer's disease.

This study identifies MSN and CD44 as potential therapeutic targets for Alzheimer's disease by developing inhibitors of their interaction through structural and chemical screening.

Large eQTL meta-analysis reveals differing patterns between cerebral cortical and cerebellar brain regions

This paper performs a large-scale eQTL meta-analysis across cerebral cortical and cerebellar brain regions, identifying distinct eQTL patterns and demonstrating improved power over existing studies.

Inhibition of the SUV4-20 H1 histone methyltransferase increases frataxin expression in Friedreich's ataxia patient cells

This study shows that inhibiting SUV4-20 H1 increases frataxin expression in FRDA cells and patient-derived cells, suggesting it as a therapeutic target.

TargetDB: A target information aggregation tool and tractability predictor

TargetDB aggregates public target information and predicts tractability to aid in drug target identification.