Cargando…

Varenicline Interactions at the 5-HT(3) Receptor Ligand Binding Site are Revealed by 5-HTBP

[Image: see text] Cys-loop receptors are the site of action of many therapeutic drugs. One of these is the smoking cessation agent varenicline, which has its major therapeutic effects at nicotinic acetylcholine (nACh) receptors but also acts at 5-HT(3) receptors. Here, we report the X-ray crystal st...

Descripción completa

Detalles Bibliográficos
Autores principales:	Price, Kerry L., Lillestol, Reidun K., Ulens, Chris, Lummis, Sarah C.R.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2015
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4505686/ https://www.ncbi.nlm.nih.gov/pubmed/25648658 http://dx.doi.org/10.1021/cn500369h

Ejemplares similares

Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT(3) receptor via a common vestibule site
por: Brams, Marijke, et al.
Publicado: (2020)

Cysteine modification reveals which subunits form the ligand binding site in human heteromeric 5-HT(3)AB receptors
por: Thompson, A J, et al.
Publicado: (2011)

Structural basis of ligand recognition in 5-HT(3) receptors
por: Kesters, Divya, et al.
Publicado: (2013)

Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor()
por: Del Cadia, Marta, et al.
Publicado: (2013)

5-Fluorotryptamine is a partial agonist at 5-HT(3) receptors, and reveals that size and electronegativity at the 5 position of tryptamine are critical for efficient receptor function
por: Bower, Kiowa S., et al.
Publicado: (2008)

High-affinity fluorescent ligands for the 5-HT(3) receptor
por: Simonin, Jonathan, et al.
Publicado: (2012)

Agonists and antagonists induce different palonosetron dissociation rates in 5-HT(3)A and 5-HT(3)AB receptors()
por: Lummis, Sarah C.R., et al.
Publicado: (2013)

Regulation of a pentameric ligand-gated ion channel by a semiconserved cationic lipid-binding site
por: Sridhar, Akshay, et al.
Publicado: (2021)

Ginkgolide B and bilobalide block the pore of the 5-HT(3) receptor at a location that overlaps the picrotoxin binding site
por: Thompson, Andrew J., et al.
Publicado: (2011)

The binding characteristics and orientation of a novel radioligand with distinct properties at 5-HT(3)A and 5-HT(3)AB receptors
por: Thompson, Andrew J., et al.
Publicado: (2014)

Discriminating between 5-HT(3)A and 5-HT(3)AB receptors
por: Thompson, AJ, et al.
Publicado: (2013)

A Hydrogen Bond in Loop A Is Critical for the Binding and Function of the 5-HT(3) Receptor
por: Price, Kerry L., et al.
Publicado: (2008)

5-HT(3) Receptors
por: Lummis, Sarah C. R.
Publicado: (2012)

Detection of human and rodent 5-HT(3B )receptor subunits by anti-peptide polyclonal antibodies
por: Reeves, David C, et al.
Publicado: (2006)

Structure–Activity Relationships of Quinoxaline-Based 5-HT(3)A and 5-HT(3)AB Receptor-Selective Ligands
por: Thompson, Andrew J, et al.
Publicado: (2013)

A single channel mutation alters agonist efficacy at 5-HT(3)A and 5-HT(3)AB receptors
por: Thompson, A J, et al.
Publicado: (2013)

5-HT(3) Receptor Brain-Type B-Subunits are Differentially Expressed in Heterologous Systems
por: Corradi, Jeremias, et al.
Publicado: (2015)

Multisite Binding of a General Anesthetic to the Prokaryotic Pentameric Erwinia chrysanthemi Ligand-gated Ion Channel (ELIC)
por: Spurny, Radovan, et al.
Publicado: (2013)

The pharmacological profile of ELIC, a prokaryotic GABA-gated receptor
por: Thompson, Andrew J., et al.
Publicado: (2012)

Design, Synthesis, and Structure–Activity Relationships of Highly Potent 5-HT(3) Receptor Ligands
por: Verheij, Mark H. P., et al.
Publicado: (2012)

Loop B Is a Major Structural Component of the 5-HT(3) Receptor
por: Thompson, A. J., et al.
Publicado: (2008)

Structural insights into the ligand binding and G(i) coupling of serotonin receptor 5-HT(5A)
por: Tan, Yangxia, et al.
Publicado: (2022)

5-HT(3) Receptor MX Helix Contributes to Receptor Function
por: Mocatta, James, et al.
Publicado: (2022)

Anxiolytic-like effects observed in rats exposed to the elevated zero-maze following treatment with 5-HT(2)/5-HT(3)/5-HT(4) ligands
por: Bell, Rob, et al.
Publicado: (2014)

Trans−cis Switching Mechanisms in Proline Analogues and Their Relevance for the Gating of the 5-HT(3) Receptor
por: Melis, Claudio, et al.
Publicado: (2009)

An atypical residue in the pore of Varroa destructor GABA-activated RDL receptors affects picrotoxin block and thymol modulation
por: Price, Kerry L., et al.
Publicado: (2014)

Identification of critical residues in loop E in the 5-HT(3AS)R binding site
por: Venkataraman, Padmavati, et al.
Publicado: (2002)

Development of Plate Reader and On-Line Microfluidic Screening to Identify Ligands of the 5-Hydroxytryptamine Binding Protein in Venoms
por: Otvos, Reka A., et al.
Publicado: (2015)

Glutamine 57 at the Complementary Binding Site Face Is a Key Determinant of Morantel Selectivity for α7 Nicotinic Receptors
por: Bartos, Mariana, et al.
Publicado: (2009)

Therapeutic Potential of 5-HT(2C) Receptor Ligands
por: Jensen, Nanna H., et al.
Publicado: (2010)

Overcoming Depression with 5-HT(2A) Receptor Ligands
por: Zięba, Agata, et al.
Publicado: (2021)

Application of Quantitative Structure–Activity Relationship Models of 5-HT(1A) Receptor Binding to Virtual Screening Identifies Novel and Potent 5-HT(1A) Ligands
por: Luo, Man, et al.
Publicado: (2014)

Could APO-varenicline and cytisine be solutions for the shortage of varenicline in Brazil?
por: Corrêa, Paulo César Rodrigues Pinto, et al.
Publicado: (2023)

An Algorithm to Identify Target-Selective Ligands – A Case Study of 5-HT7/5-HT1A Receptor Selectivity
por: Kurczab, Rafał, et al.
Publicado: (2016)

Classification of 5-HT(1A) Receptor Ligands on the Basis of Their Binding Affinities by Using PSO-Adaboost-SVM
por: Cheng, Zhengjun, et al.
Publicado: (2009)

New Triazine Derivatives as Serotonin 5-HT(6) Receptor Ligands
por: Łażewska, Dorota, et al.
Publicado: (2023)

Distribution of 5-HT(3), 5-HT(4), and 5-HT(7) Receptors Along the Human Colon
por: Yaakob, Nor S, et al.
Publicado: (2015)

Identification of novel α7 nicotinic receptor ligands by in silico screening against the crystal structure of a chimeric α7 receptor ligand binding domain
por: Akdemir, Atilla, et al.
Publicado: (2012)

Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H(4) and the ion channel serotonin 5-HT(3A)
por: Verheij, Mark H.P., et al.
Publicado: (2011)

Review: 5-HT(1), 5-HT(2), 5-HT(3) and 5-HT(7) Receptors and their Role in the Modulation of Pain Response in the Central Nervous System
por: Cortes-Altamirano, Jose Luis, et al.
Publicado: (2018)

Cannot write session to /tmp/vufind_sessions/sess_itgd56b1jgqpaeg8ereftht6bt