Literature DB >> 24328812

The tail wags the dog: possible mechanism for reverse allosteric control of ligand-activated channels.

E Vardy1, T Kenakin.   

Abstract

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.
© 2013 The British Pharmacological Society.

Entities:  

Keywords:  5-HT3; allostery; ion channels; serotonin

Mesh:

Substances:

Year:  2014        PMID: 24328812      PMCID: PMC3966742          DOI: 10.1111/bph.12550

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  8 in total

1.  A cytoplasmic region determines single-channel conductance in 5-HT3 receptors.

Authors:  Stephen P Kelley; James I Dunlop; Ewen F Kirkness; Jeremy J Lambert; John A Peters
Journal:  Nature       Date:  2003-07-17       Impact factor: 49.962

2.  Refined structure of the nicotinic acetylcholine receptor at 4A resolution.

Authors:  Nigel Unwin
Journal:  J Mol Biol       Date:  2005-01-25       Impact factor: 5.469

Review 3.  Structural insights into Cys-loop receptor function and ligand recognition.

Authors:  Mieke Nys; Divya Kesters; Chris Ulens
Journal:  Biochem Pharmacol       Date:  2013-07-10       Impact factor: 5.858

Review 4.  Physiology and pathophysiology of the 5-HT3 receptor.

Authors:  L Färber; U Haus; M Späth; S Drechsler
Journal:  Scand J Rheumatol Suppl       Date:  2004

5.  Evidence for the existence of 5-hydroxytryptamine receptors, which are not of the 5-HT2 type, mediating contraction of rabbit isolated basilar artery.

Authors:  P B Bradley; P P Humphrey; R H Williams
Journal:  Br J Pharmacol       Date:  1986-01       Impact factor: 8.739

6.  Two kinds of tryptamine receptor.

Authors:  J H GADDUM; Z P PICARELLI
Journal:  Br J Pharmacol Chemother       Date:  1957-09

7.  The Concise Guide to PHARMACOLOGY 2013/14: ligand-gated ion channels.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

8.  Impact of intracellular domain flexibility upon properties of activated human 5-HT3 receptors.

Authors:  J L Kozuska; I M Paulsen; W J Belfield; I L Martin; D J Cole; A Holt; S M J Dunn
Journal:  Br J Pharmacol       Date:  2014-04       Impact factor: 8.739

  8 in total
  1 in total

Review 1.  Serotonin, neural markers, and memory.

Authors:  Alfredo Meneses
Journal:  Front Pharmacol       Date:  2015-07-21       Impact factor: 5.810

  1 in total

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