Publications by authors named "Gilana Reiss"
Article Synopsis
- * Peptidases are identified as potential drug targets in the Plasmodium falciparum lifecycle, specifically two metallo-aminopeptidases (MAPs), PfA-M1 and Pf-LAP, which are crucial for the parasite's survival.
- * By creating targeted activity-based probes, researchers discovered that inhibiting PfA-M1 disrupts hemoglobin processing and leads to parasite death, while inhibiting Pf-LAP is lethal at an earlier stage, indicating its vital role in the parasite's lifecycle before hemoglobin degradation.
A novel set of activity-based probes (ABPs) for functionally profiling metallo-aminopeptidases was synthesized based on the bestatin inhibitor scaffold, the first synthesis of bestatin analogues using solid-phase techniques. These ABPs were shown to label metallo-aminopeptidases, using both a biotin and a fluorophore reporter, in an activity-dependent manner. This probe class was also shown to be amenable to 'click' chemistry labeling for possible use in live cells.
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