T. Kronenberger

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.

Beyond the MEP Pathway: a novel kinase required for prenol utilization by malaria parasites

This study identifies a novel kinase in malaria parasites that enables prenol salvage, showing its role in bypassing MEP pathway inhibition and enhancing drug efficacy.

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.

HilE represses the activity of HilD via a mechanism distinct from that of intestinal long-chain fatty acids.

This study identifies two distinct mechanisms by which HilD activity is repressed: LCFAs bind to a conserved pocket, while HilE forms a heterodimer with HilD.

Structure-based identification of naphthoquinones and derivatives as novel inhibitors of main protease Mpro and papain-like protease PLpro of SARS-CoV-2

This study identifies naphthoquinone derivatives as inhibitors of SARS-CoV-2 proteases Mpro and PLpro through virtual screening and biochemical assays.

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.