L. M. Berger

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.

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.

A Highly Selective Chemical Probe for Activin Receptor-like Kinases ALK4 and ALK5

The paper develops a selective chemical probe, TP-008, for ALK4 and ALK5 kinases and provides a negative control, enabling mechanistic studies of their signaling pathway and disease roles.