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...

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Bibliographic Details
Published inFarmaco (Società chimica italiana : 1989) Vol. 55; no. 3; pp. 202 - 205
Main Author Usherwood, Peter N.R
Format Journal Article
LanguageEnglish
Published France Elsevier SAS 01.03.2000
Subjects
Animals
Biogenic Polyamines - pharmacology
Humans
Ion Channels - antagonists & inhibitors
Neurotoxins
Polyamines
Polyamines - pharmacology
Protein Sorting Signals - physiology
Receptors, Cell Surface - drug effects
Signal Transduction - drug effects
Signalling proteins
Signalling proteins
Polyamines
Neurotoxins
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Summary: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.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
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ObjectType-Review-1
ISSN:0014-827X
1879-0569
DOI:10.1016/S0014-827X(00)00023-9