Natural and synthetic polyamines: modulators of signalling proteins.
Ionotropic receptors are modulated allosterically by natural polyamines, such as spermine, and by polyamine derivatives, such as polyamine amides (e.g. philanthotoxin-343) and polymethylene tetraamines (e.g. methoctramine. Modulation can be either positive (potentiation) or negative (non-competitive antagonism of either open or closed channel receptor conformation). Photoaffinity labelling studies have identified a site close to the channel lumen on the nicotinic acetylcholine receptor Torpedo electroplax that is probably the allosteric site responsible for antagonism of the closed channel conformation of this receptor.
Division of Molecular Toxicology, School of Biological Sciences, University of Nottingham, UK.
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Usherwood
D000818:Animals; D015317:Biogenic Polyamines / Q000494:pharmacology*; D006801:Humans; D007473:Ion Channels / Q000037:antagonists & inhibitors; D011073:Polyamines / Q000494:pharmacology*; D021382:Protein Sorting Signals / Q000502:physiology*; D011956:Receptors, Cell Surface / Q000187:drug effects; D015398:Signal Transduction / Q000187:drug effects*
D015317:Biogenic Polyamines; D007473:Ion Channels; D011073:Polyamines; D021382:Protein Sorting Signals; D011956:Receptors, Cell Surface