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The tail wags the dog: possible mechanism for reverse allosteric control of ligand‐activated channels
Author(s) -
Vardy E,
Kenakin T
Publication year - 2014
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.12550
Subject(s) - allosteric regulation , cooperativity , receptor , chemistry , biophysics , intracellular , ligand (biochemistry) , biology , biochemistry
In this issue of the British Journal of Pharmacology, a new article by Kozuska et al. discusses the multiple salt bridges in the intracellular domain of the 5HT3A receptor. These interactions increase the overall rigidity of the receptor, stabilize its low conducting state and affect the ligand cooperativity. The authors suggest that the allosteric effects of these regions on the receptor may be involved in a possible 'reverse' allosteric modulation of 5HT3 receptors.