Publications by authors named "B Deprez"
Among the M1 family of oxytocinase aminopeptidases, insulin-regulated aminopeptidase IRAP, is an emerging drug target implicated in various biological pathways and particularly in MHC-I antigen presentation through amino-terminal trimming of exogenous cross-presented peptides. A few series of inhibitors inspired either by angiotensin IV, one of IRAP substrates, or by bestatin a pan aminopeptidase inhibitor, have been disclosed. However, the variety and number of chemotypes remains relatively limited.
View Article and Find Full Text PDFIntroduction: Inflammatory bowel diseases (IBDs) are chronic immune driven intestinal disorders with marked metabolic alteration. Mass spectrometry imaging (MSI) enables the direct visualization of biomolecules within tissues and facilitates the study of metabolic changes. Integrating multiple spatial information sources is a promising approach for discovering new biomarkers and understanding biochemical alteration within the context of the disease.
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- * Researchers synthesized triazole-containing compounds that showed strong antibacterial effects, especially one named BDM71403, which was found to be more effective than the reference drug, gepotidacin.
- * Detailed structural studies using cryo-electron microscopy revealed how BDM71403 interacts with DNA gyrase and DNA, providing insights for future antibiotic development to combat resistant bacteria.
Article Synopsis
- Researchers identified multiple ERAP1 inhibitors using a fragment-based screening approach from a library of around 3000 compounds, resulting in 32 potential candidates.
- The team optimized three specific chemical structures, leading to two types of compounds with effective inhibition and selectivity against a related enzyme, which could pave the way for future drug development.