Thank you @helloeacr.bsky.social for highlighting our work on KRAS dregarders #TPD #KRAS in EACR‘s Highlights in Cancer Research

Great to see our First Disclosure of Brigimadlin, a highly potent MDM2 inhibitor highlighted and on the cover of Molecular Cancer Therapeutics @theaacr.bsky.social aacrjournals.org/mct/article/.... Congratulations to the team at @boehringer.bsky.social

Covalent targeting of splicing in T cells Despite significant interest in therapeutic targeting of splicing, few chemical probes are available for the proteins involved in splicing. Here, we s…

New paper out of Katya Vinogradova’s lab! www.sciencedirect.com/science/arti...

Hi Scott, would be great if you could add me!

Hi Jordon, thank you for putting together this list! It would be great if you could add me.

Welcome to Bluesky! I created a starter pack for medicinal chemistry. Please comment/share and let me know if you wish to be added to the starter pack.

go.bsky.app/8JRwAao

Discovery and Preclinical Characterization of Fulacimstat (BAY 1142524), a Potent and Selective Chymase Inhibitor As a New Profibrinolytic Approach for Safe Thrombus Resolution Chymase is a serine-protease produced by mast cells. In the past few decades, its role in fibrotic diseases triggered the search for orally available chymase inhibitors. Aiming at reducing adverse cardiac remodeling after myocardial infarction, our research efforts resulted in the discovery of fulacimstat (BAY 1142524). While clinical trials did not demonstrate efficacy in this indication, the recent discovery of a new unexpected biological role of chymase spurred a revival of interest in chymase inhibition: chymase was shown to inactivate plasmin within fibrin-rich clots. Chymase inhibitors are now considered as potential profibrinolytic drugs with low bleeding risk and therefore exceptional safety for the treatment of acute thrombosis settings such as stroke, pulmonary embolism, or venous thrombosis. This article describes the chemical optimization journey from a screening hit to the discovery of fulacimstat (BAY 1142524), a selective chymase inhibitor with a good safety profile, as well as its preclinical in vitro and in vivo characterization.

Great in-depth work by C. Fürstner and colleagues at Bayer on chymase inhibitor Fulacimstat. Optimization starting from sub-optimal screening hit yielding a promising candidate. Including extensive SAR, X-rays and early tox data. Congrats!

pubs.acs.org/doi/10.1021/...

Hi Sean, thank you for putting together this list, it would be great if you could add me.