title: PARtitioning protease signaling.
abstract: In this issue of Blood, Aisiku et al describe a novel class of protease-activated receptor-1 (PAR1) inhibitors that block proinflammatory pathways but spare cytoprotective signaling in endothelial cells. These compounds, parmodulins, target the cytoplasmic face of PAR1, where they selectively interfere with Gαq, but not Gα12/13. This strategy of blocking specific pathways provides the ability to modulate the activity of receptors with multiple functions (such as PAR1) and may have therapeutic advantages.
authors: CASE WESTERN RESERVE UNIVERSITY.
authors: Marvin T
authors: http://orcid.org/0000-0003-2602-023X
authors: MT
authors: Nieman
mesh_terms: D000818:Animals; D004730:Endothelium, Vascular / Q000293:injuries*; D006801:Humans; D007783:Lactones / Q000009:adverse effects*; D011725:Pyridines / Q000009:adverse effects*; D013927:Thrombosis / Q000188:drug therapy* / Q000517:prevention & control*; D010975:Platelet Aggregation Inhibitors
chemical_list: D007783:Lactones; D011725:Pyridines; C530299:vorapaxar; D010975:Platelet Aggregation Inhibitors