Monday, January 15, 2024

Diazepam-based covalent modifiers of GPX4 induce ferroptosis in liver cancer cells

D. Yadav, S. Tiwari, S. Senthil, S. K. Vechalapu, S. Duraisamy, V. Rawat, M. I. Rahman, S. Khanna and D. Allimuthu, 

Chem. Commun., 2024

DOI: 10.1039/D3CC06215E

Developing new chemotherapeutics that are structurally and mechanistically unique is a need due to the rapid rise of cancer incidences across the globe. Here we report the identification of irreversible, thiol-reactive diazepam derivatives as GPX4 modifiers and nanomolar inducers of ferroptosis in liver cancer cells.



Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis

Martin K. Himmelbauer, Bekim Bajrami, Rebecca Basile, Andrew Capacci, TeYu Chen, Colin K. Choi, Rab Gilfillan, Felix Gonzalez-Lopez de Turis...