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Adv Protein Chem Struct Biol. 2016;104:39-79. doi: 10.1016/bs.apcsb.2015.11.004. Epub 2016 Jan 4.

P2X7 Receptor as a Therapeutic Target.

Author information

1
Department of Morphology, Surgery and Experimental Medicine, Section of Pathology, Oncology and Experimental Biology, University of Ferrara, Ferrara, Italy.
2
School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy.
3
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.

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.

KEYWORDS:

ATP; Cancer; Inflammation; Ligands; Mood disorders; Neurodegeneration; Osteoporosis; P2X7; SNPs

PMID:
27038372
DOI:
10.1016/bs.apcsb.2015.11.004
[Indexed for MEDLINE]

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