A Hydrogen Bond in Loop A Is Critical for the Binding and Function of the 5-HT3 Receptor

KL Price, KS Bower, AJ Thompson, HA Lester… - Biochemistry, 2008 - ACS Publications
The binding sites of Cys-loop receptors are formed from at least six loops (A− F). Here we
have used mutagenesis, radioligand binding, voltage clamp electrophysiology, and …

[HTML][HTML] Locating an antagonist in the 5-HT3 receptor binding site using modeling and radioligand binding

AJ Thompson, KL Price, DC Reeves, SL Chan… - Journal of biological …, 2005 - ASBMB
We have used a homology model of the extracellular domain of the 5-HT 3 receptor to dock
granisetron, a 5-HT 3 receptor antagonist, into the binding site using AUTODOCK. This …

Interactions of Granisetron with an Agonist-Free 5-HT3A Receptor Model

PR Joshi, A Suryanarayanan, E Hazai, MK Schulte… - Biochemistry, 2006 - ACS Publications
A new homology model of type-3A serotonin receptors (5-HT3ARs) was built on the basis of
the electron microscopic structure of the nicotinic acetylcholine receptor and with an agonist …

[HTML][HTML] A single mutation in the 5-HT4 receptor (5-HT4-R D100 (3.32) A) generates a Gs-coupled receptor activated exclusively by synthetic ligands (RASSL)

S Claeysen, L Joubert, M Sebben, J Bockaert… - Journal of Biological …, 2003 - ASBMB
To better understand G-protein-coupled receptor (GPCRs) signaling, cellular and animal
physiology, as well as gene therapy, a new tool has recently been proposed. It consists of …

Spatial orientation of the antagonist granisetron in the ligand-binding site of the 5-HT3 receptor

D Yan, MM White - Molecular pharmacology, 2005 - ASPET
The serotonin type 3 receptor (5-HT3R) is a member of the cys-loop ligand-gated ion
channel (LGIC) superfamily. Like almost all membrane proteins, high-resolution structural …

Defining the roles of Asn-128, Glu-129 and Phe-130 in loop A of the 5-HT3 receptor

NL Sullivan, NL Sullivan, AJ Thompson… - Molecular membrane …, 2006 - Taylor & Francis
The ligand binding pocket of Cys-loop receptors consists of a number of binding loops
termed A–F. Here we examine the 5-HT3 receptor loop A residues Asn-128, Glu-129 and …

[HTML][HTML] Loop B is a major structural component of the 5-HT3 receptor

AJ Thompson, M Lochner, SCR Lummis - Biophysical journal, 2008 - cell.com
The 5-HT 3 receptor belongs to a family of therapeutically important neurotransmitter-gated
receptors whose ligand binding sites are formed by the convergence of six peptide loops …

[HTML][HTML] Mutagenesis and molecular modeling reveal the importance of the 5-HT3 receptor F-loop

AJ Thompson, CL Padgett, SCR Lummis - Journal of biological chemistry, 2006 - ASBMB
The 5-HT 3 receptor is a member of the Cys-loop family of ligandgated ion channels. The
extracellular domains of these proteins contain six amino acid loops (A–F) that converge to …

New insights into the human 5‐HT4 receptor binding site: exploration of a hydrophobic pocket

L Rivail, M Giner, M Gastineau… - British journal of …, 2004 - Wiley Online Library
A body of evidences suggests that a hydrophobic pocket of the human 5‐HT4 receptor
contributes to the high affinity of some bulky 5‐HT4 ligands. A thorough study of this pocket …

[HTML][HTML] Functional group interactions of a 5-HT3R antagonist

P Venkataraman, P Joshi, SP Venkatachalan… - BMC biochemistry, 2002 - Springer
Background Lerisetron, a competitive serotonin type 3 receptor (5-HT 3 R) antagonist,
contains five functional groups capable of interacting with amino acids in the 5-HT 3 R …