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Protease-activated receptors in health and disease.
Peach, Chloe J; Edgington-Mitchell, Laura E; Bunnett, Nigel W; Schmidt, Brian L.
Affiliation
  • Peach CJ; Department of Molecular Pathobiology, College of Dentistry, New York University, New York, New York.
  • Edgington-Mitchell LE; Department of Neuroscience and Physiology and Neuroscience Institute, Grossman School of Medicine, New York University, New York, New York.
  • Bunnett NW; Department of Biochemistry and Pharmacology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Parkville, Victoria, Australia.
  • Schmidt BL; Bluestone Center for Clinical Research, Department of Oral and Maxillofacial Surgery, New York University College of Dentistry, New York, New York.
Physiol Rev ; 103(1): 717-785, 2023 01 01.
Article in En | MEDLINE | ID: mdl-35901239
Proteases are signaling molecules that specifically control cellular functions by cleaving protease-activated receptors (PARs). The four known PARs are members of the large family of G protein-coupled receptors. These transmembrane receptors control most physiological and pathological processes and are the target of a large proportion of therapeutic drugs. Signaling proteases include enzymes from the circulation; from immune, inflammatory epithelial, and cancer cells; as well as from commensal and pathogenic bacteria. Advances in our understanding of the structure and function of PARs provide insights into how diverse proteases activate these receptors to regulate physiological and pathological processes in most tissues and organ systems. The realization that proteases and PARs are key mediators of disease, coupled with advances in understanding the atomic level structure of PARs and their mechanisms of signaling in subcellular microdomains, has spurred the development of antagonists, some of which have advanced to the clinic. Herein we review the discovery, structure, and function of this receptor system, highlight the contribution of PARs to homeostatic control, and discuss the potential of PAR antagonists for the treatment of major diseases.
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Full text: 1 Database: MEDLINE Main subject: Signal Transduction / Receptors, Proteinase-Activated Limits: Humans Language: En Year: 2023 Type: Article

Full text: 1 Database: MEDLINE Main subject: Signal Transduction / Receptors, Proteinase-Activated Limits: Humans Language: En Year: 2023 Type: Article