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Proteinase‐activated receptor 2 (PAR‐2) is a G protein–coupled receptor activated by both trypsin and a specific agonist peptide, SLIGKV‐NH2. It has been linked to various pathologies, including pain and inflammation. Several peptide and peptidomimetic agonizts for PAR‐2 have been developed exhibiting high potency and efficacy. However, the number of PAR‐2 antagonists is smaller. We screened the Food...
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