title: P2X7 Receptor as a Therapeutic Target.
abstract: P2X7 receptor is an ATP-gated cation channel that upon agonist interaction leads to cellular influx of Na(+) and Ca(2+) and efflux of K(+). P2X7 is expressed by a wide variety of cells and its activation mediates a large number of biological processes like inflammation, neuromodulation, cell death or cell proliferation and it has been associated to related pathological conditions including infectious, inflammatory, autoimmune, neurological, and musculoskeletal disorders and, in the last years, to cancer. This chapter describes structural features of P2X7, chemical properties of its agonist, antagonist, and allosteric modulators and summarizes recent advances on P2X7 receptor as therapeutic target in the aforementioned diseases. We also give an overview on recent literature suggesting that P2X7 single-nucleotide polymorphisms could be exploited as diagnostic biomarkers for the development of tailored therapies.
authors.affiliation: Department of Morphology, Surgery and Experimental Medicine, Section of Pathology, Oncology and Experimental Biology, University of Ferrara, Ferrara, Italy.
authors.forename: Elena
authors.initials: E
authors.lastname: De Marchi
authors.affiliation: Department of Morphology, Surgery and Experimental Medicine, Section of Pathology, Oncology and Experimental Biology, University of Ferrara, Ferrara, Italy.
authors.forename: Elisa
authors.initials: E
authors.lastname: Orioli
authors.affiliation: School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy.
authors.forename: Diego
authors.initials: D
authors.lastname: Dal Ben
authors.affiliation: Department of Morphology, Surgery and Experimental Medicine, Section of Pathology, Oncology and Experimental Biology, University of Ferrara, Ferrara, Italy. Electronic address: elena.adinolfi@unife.it.
authors.forename: Elena
authors.initials: E
authors.lastname: Adinolfi
mesh_terms: D006801:Humans; D007239:Infections / Q000188:drug therapy* / Q000473:pathology; D007249:Inflammation / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D008024:Ligands; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D010024:Osteoporosis / Q000188:drug therapy / Q000473:pathology; D058911:Purinergic P2X Receptor Agonists / Q000627:therapeutic use; D058920:Purinergic P2X Receptor Antagonists / Q000627:therapeutic use; D058486:Receptors, Purinergic P2X7 / Q000235:genetics* / Q000378:metabolism
chemical_list: D008024:Ligands; C546468:P2RX7 protein, human; D058911:Purinergic P2X Receptor Agonists; D058920:Purinergic P2X Receptor Antagonists; D058486:Receptors, Purinergic P2X7
keywords: ATP; Cancer; Inflammation; Ligands; Mood disorders; Neurodegeneration; Osteoporosis; P2X7; SNPs