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Publications
All publications
Targeting the Membrane-Embedded Rhomboid Protease GlpG: A Multimodal Strategy for Inhibitor Discovery and Mechanistic Insight
Angewandte Chemie International Edition 65 (10): e14067 (2026)
Rhomboid proteases, a class of intramembrane proteases characterized by a Ser-His catalytic dyad, have recently emerged as promising therapeutic targets. While inhibitors for soluble serine proteases have been extensively studied, the spectrum of potent rhomboid protease inhibitor chemotypes is limited to active-site targeted nucleophiles. To address this limitation, we conducted a high-throughput screen of over 68,000 compounds targeting the E. coli rhomboid protease GlpG, using a fluorescent liposome-based assay. A selection of 326 inhibitory compounds was evaluated in a subsequent IC50 screen against two variants of GlpG (core domain and full length), a soluble serine protease (chymotrypsin), as well as the human mitochondrial rhomboid PARL. Of these, the selective inhibitory effects of 2 compounds and their analogues on GlpG were confirmed through further biochemical and biophysical characterisation, molecular docking, and solid-state NMR spectroscopy. This study paves the way for…
Steroidal hormones and neurosteroids - novel therapeutic strategies in bacterial infections: Design, synthesis, and biological evaluation
European Journal of Medicinal Chemistry 308: 118716 (2026)
Efficient Method for High-Throughput Screening of Compound Libraries Targeting Human PD-L1
ACS Omega 11 (13): 20626–20635 (2026)
Total Synthesis of (+)-Malbrancheamide B Employing a Bioinspired Strategy
Organic Letters 28 (10): 3214–3219 (2026)