Orthosteric and allosteric binding sites of P2X receptors

P2X receptors for ATP comprise a distinct family of ligand gated ion channels with a range of properties. They have been shown to be involved in a variety of physiological processes including blood clotting, sensory perception, pain sensation, bone formation as well as inflammation and may provide a...

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Bibliographic Details
Published in:European biophysics journal 2009-03, Vol.38 (3), p.319-327
Main Author: Evans, R. J
Format: Article
Language:English
Subjects:
Adenosine Triphosphate - metabolism
Allosteric Site
Amino Acid Sequence
Animals
ATP
Binding Sites
Biochemistry
Biological and Medical Physics
Biomedical and Life Sciences
Biophysics
Cell Biology
Humans
Ion Channel Gating - physiology
Life Sciences
Membrane Biology
Models, Molecular
Molecular Sequence Data
Nanotechnology
Neurobiology
Pharmacology
Protein Conformation
Receptors, Purinergic P2 - physiology
Receptors, Purinergic P2X
Review
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Description
Summary:P2X receptors for ATP comprise a distinct family of ligand gated ion channels with a range of properties. They have been shown to be involved in a variety of physiological processes including blood clotting, sensory perception, pain sensation, bone formation as well as inflammation and may provide a number of novel drug targets. In addition to the orthosteric site for ATP binding it has been suggested that there may be additional allosteric sites that regulate agonist action at the receptor. There is currently no crystal structure available for P2X receptors and the lack of sequence similarity to other ATP binding proteins has meant that a mutagenesis-based approach has been used primarily to investigate receptor structure-function. This review aims to provide an overview of recent work that gives an insight into residues involved in ATP action and allosteric regulation.
ISSN:0175-7571
1432-1017
DOI:10.1007/s00249-008-0275-2