Lewis Elson

The paper describes the development of AZ137, a potent and selective HIPK4 inhibitor derived from bosutinib, and validates its utility as a tool for studying HIPK4's biological functions.

This study develops peptide-based tracers for SPSB2 E3 ligase by conjugating cell-penetrating peptides to degrons, enabling efficient cellular delivery and target engagement assessment.

The paper describes the optimization of a macrocyclic scaffold to develop a selective STK10 inhibitor with nanomolar activity and good kinome selectivity.

This study develops a covalent LIMK1 inhibitor that selectively targets a unique cysteine, enabling isoform-specific studies of LIMK1 function.

Hybrid type-II inhibitors RN277 and RN341 target inactive LRRK2 with far fewer kinase off-targets than Rebastinib, preserve S935 phosphorylation, and rescue kinesin motility in vitro.

The paper repurposes a benzoxazepinone scaffold originally designed for RIPK1 inhibition to develop a novel type-III LIMK1/2 inhibitor with high selectivity.

The paper evaluates diverse ubiquitin pathway inhibitors as controls for CRBN and VHL-mediated protein degradation, assessing their potency and toxicity using the HiBiT system and high content assays.

The paper optimizes a 2-aminopyrimidine-based macrocycle to create a dual EPHA2/GAK kinase inhibitor with antiviral activity against dengue virus.

The paper designs and evaluates chemical linchpins targeting CK2α with a novel binding mode combining allosteric and ATP competitive elements, showing high selectivity and low micromolar activity.

This study develops selective MST3/4 kinase inhibitors and demonstrates their distinct cellular effects compared to MST1/2 inhibition.

The paper designs and synthesizes a macrocyclic inhibitor, JA310, that selectively targets MST3 with high potency and kinome-wide selectivity.