A. Kraemer

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.

STIL overexpression shortens lifespan and reduces tumor formation in mice

This study shows that STIL overexpression increases centrosome numbers, leading to aneuploidy and reduced tumor formation and lifespan in mice.

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.

5-iodotubercidin sensitizes cells to RIPK1-dependent necroptosis by interfering with NFkappaB signaling

This study identifies 5-iodotubercidin as a compound that sensitizes cells to RIPK1-dependent necroptosis by inhibiting NFκB signaling in MK2-deficient cells.

Design, Synthesis and Evaluation of WD-repeat containing protein 5 (WDR5) degraders

This study designs, synthesizes, and evaluates two series of WDR5 degraders, showing that linker length and nature affect degradation efficacy.

The evolution of trait variance creates a tension between species diversity and functional diversity

The paper shows that increased species diversity can reduce functional diversity due to evolutionary pressures for narrower trait variation in competitive communities.

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.