PZ-235

PZ-235 is a first-in-class pepducin designed to selectively antagonize Protease-Activated Receptor 2 (PAR2), a G protein-coupled receptor (GPCR) that is a key mediator of inflammation, pain, and pruritus. Developed by Oasis Pharmaceuticals, PZ-235 utilizes proprietary pepducin technology, which consists of a cell-penetrating lipopeptide derived from the intracellular loops of the target receptor. Unlike traditional orthosteric antagonists, PZ-235 crosses the cell membrane to target the intracellular face of PAR2, effectively blocking G-protein signaling from the inside out. This mechanism allows for potent inhibition of inflammatory cascades triggered by proteases such as trypsin and mast cell tryptase. PZ-235 has been investigated for its therapeutic potential in treating inflammatory skin conditions like atopic dermatitis, as well as other PAR2-driven pathologies including asthma and certain cancers.

Other names

PAR2 pepducinPAR-2 pepducinPAR 2 pepducinProtease-activated receptor 2 pepducin