Molecular mechanisms regulating Proteinase?Activated Receptors (PARs)

Proteinase-activated receptors (PARs) are a four-member family of G protein-coupled defined by their irreversible proteolytic mechanism activation. PARs have emerged as important regulators various physiological responses and implicated in numerous pathological conditions. Importantly, PAR1 PAR4 critical platelet function, while PAR2 is well established driver inflammatory responses. PAR-targeted drug development efforts therefore great interest. In this review, we provide an overview recent advances our understanding molecular mechanisms underlying PAR activation, effector interaction, signaling. We also the diverse enzymes that now describe ability different to elicit biased signaling through PARs. Finally, highlight pharmacological agents discuss structure–activity relationship studies.