A. C. Joerger

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.

Development of potent dual BET/HDAC inhibitors via pharmacophore merging and structure-guided optimization

This study develops potent dual BET/HDAC inhibitors through pharmacophore merging and structure-guided optimization, showing improved potency and efficacy in cancer cell models.

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.

Functional diversity of the TP53 mutome revealed by saturating CRISPR mutagenesis

This study uses CRISPR mutagenesis to analyze the functional impact of TP53 mutations across 9,225 variants, revealing their effects on tumor cell fitness and metastasis.

Structure-based design of selective salt-inducible kinase (SIK) inhibitors

This study designs a selective SIK inhibitor, MRIA9, based on a PAK inhibitor, showing its dual activity and potential for combination therapy in ovarian cancer.