Author

Gabriel M. Simon

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Open access Aug 2026

Activity-based profiling of primary brain cells identifies covalent allosteric modulators of HCN channels

Chemical proteomics can provide global portraits of small molecule-protein interactions in native biological systems. Such ligandability maps have, however, been mostly restricted to readily accessible cell lines and primary immune cells. Here, we describe an activity-based protein profiling (ABPP) strategy for mapping...

Elva Ye, Alberto Russo, Roberta Castelli et al. · bioRxiv · 0 citations

Review Open access Aug 2026

Chemoproteomic discovery of a brain-penetrant, covalent NLRP3 inhibitor that binds a novel allosteric pocket.

Optimization of ligands targeting Cys463 of NLRP3 within a previously uncharacterized allosteric pocket led to a unique and potent inhibitor series with attractive physicochemical and pharmacokinetic properties for the potential treatment of diseases involving aberrant innate immune activation in both central and perip...

Donald C. Rogness, E. Sievert, Vincent F Vartabedian et al. · British Journal of Pharmacol... · 1 citation