L. Elson

Functional characterization of pathway inhibitors for the ubiquitin-proteasome system (UPS) as tool compounds for CRBN and VHL-mediated targeted protein degradation

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.

Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting

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.

Back-pocket optimization of 2-aminopyrimidine-based macrocycles leads to potent dual EPHA2/GAK kinase inhibitors with antiviral activity

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

Development of selective pyridopyrimidin-7(8H)-one-based Mammalian STE20-like (MST3/4) kinase inhibitors

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

Synthesis of pyrazole-based macrocycles leads to a highly selective inhibitor for MST3

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

Shifting the selectivity of pyridopyrimidin-7(8H)-one inhibitors towards the salt-inducible kinase (SIK) subfamily

This paper develops a selective SIK kinase inhibitor, MR22, by optimizing a pyrido[2,3-d]pyrimidin-7(8H)-one scaffold to eliminate PAK activity, demonstrating its efficacy in ovarian cancer cells.