B.-T. Berger

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.

Death by a Thousand Cuts -- Combining Kinase Inhibitors for Selective Target Inhibition and Rational Polypharmacology

This paper presents a method to improve kinase inhibitor selectivity by combining inhibitors with divergent off-target activities, validated using a NanoBRET assay.

Mutation in Abl kinase with altered drug binding kinetics indicates a novel mechanism of imatinib resistance

The paper identifies a mutation in Abl kinase that causes imatinib resistance through altered drug dissociation kinetics rather than reduced binding affinity.

Optimization of pyrazolopyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor

This paper describes the optimization of pyrazolopyrimidine compounds to develop a highly selective and potent CK2 inhibitor, IC20, with high in vitro potency and exclusive selectivity.

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.

SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)

The paper describes SGC-GAK-1, a selective GAK inhibitor, and identifies a related compound that inhibits RIPK2 without GAK activity, providing tools to study GAK and RIPK2 biology.