Structural insights into the lipid and ligand regulation of serotonin receptors.
- Biology, ChemistryNature
The results address a long-standing question of how lipids and water molecules regulate G-protein-coupled receptors, reveal how 5-HT acts as a pan-agonist, and identify the determinants of drug recognition in 5- HT receptors.
5-HT(3) receptors: role in disease and target of drugs.
- BiologyPharmacology & therapeutics
Targeting the 5-HT2C Receptor in Biological Context and the Current State of 5-HT2C Receptor Ligand Development.
- Biology, PsychologyCurrent topics in medicinal chemistry
In recent years, efforts towards developing other mechanisms to enhance receptor function have resulted in the discovery of positive allosteric modulators (PAMs) for the 5-HT2CR, with several molecule series now reported.
Approaching the 5-HT3 receptor heterogeneity by computational studies of the transmembrane and intracellular domains
- Biology, ChemistryJournal of Computer-Aided Molecular Design
3D homology models of the transmembrane and the intracellular receptor domains of all the known human 5-HT3 subunits have been built and assembled and comparative analyses of sequences, modelled structures, and computed electrostatic properties of the single subunits and of the assembled pentamers shed new light on the stoichiometric composition and on the physicochemical requirements of the functional receptors.
Bivalent Ligands for the Serotonin 5-HT3 Receptor.
- Biology, ChemistryACS medicinal chemistry letters
The high affinity shown by homobivalent ligands suggests that bivalency is a promising approach in 5-HT3 receptor modulation and provides the rational basis for applying the concepts of multivalency to the study of 5- HT3 receptor function.
5-Hydroxytryptamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
- BiologyIUPHAR/BPS Guide to Pharmacology CITE
Unique amongst the GPCRs, RNA editing produces 5-HT2C receptor isoforms that differ in function, such as efficiency and specificity of coupling to Gq/11 and also pharmacology [40, 482].
Ligand-specific differential regulation of 5-hydroxytryptamine receptors: functional selectivity in serotonergic signaling
Ligands at receptors for the biogenic amine serotonin (5-hydroxytryptamine, 5-HT) have provided convincing examples of functional selectivity, and key experiments from this area are the subject of the present review.
SHOWING 1-10 OF 222 REFERENCES
Molecular, pharmacological and functional diversity of 5-HT receptors
- BiologyPharmacology Biochemistry and Behavior
Molecular biology and potential functional role of 5-HT5, 5-HT6, and 5-HT7 receptors
This review focuses on the structural features, binding properties, and mRNA distribution of these novel 5-HT receptor subtypes, as well as an evaluation of the tool sets available to link these cloned receptors to function and therapeutic potential.
The 5-HT3B subunit is a major determinant of serotonin-receptor function
Surprisingly, the M2 region of the 5-HT3B subunit lacks any of the structural features that are known to promote the conductance of related receptors, and will be a valuable resource for defining the molecular mechanisms of ion-channel function.
Molecular pharmacology and biology of 5-HT1C receptors.
- Biology, ChemistryTrends in pharmacological sciences
Co-expression of the 5-HT3B serotonin receptor subunit alters the biophysics of the 5-HT3 receptor.
- Biology, ChemistryBiophysical journal
Receptor subtype and density determine the coupling repertoire of the 5-HT2 receptor subfamily.
- Biology, ChemistryLife sciences
The 5-hydroxytryptamine type 3 (5-HT3) receptor reveals a novel determinant of single-channel conductance.
- BiologyBiochemical Society transactions
The present study describes a novel determinant of single-channel conductance, out with the M2 domain, which accounts for this anomaly and indicates an important and hitherto unappreciated function for the HA stretch in the Cys-loop family of transmitter-gated ion channels.
Regulation of serotonin-2C receptor G-protein coupling by RNA editing
Observations indicate that RNA editing is a new mechanism for regulating serotonergic signal transduction and suggest that this post-transcriptional modification may be critical for modulating the different cellular functions that are mediated by other members of the G-protein-coupled receptor superfamily.
The Pharmacological and Functional Characteristics of the Serotonin 5-HT3A Receptor Are Specifically Modified by a 5-HT3B Receptor Subunit*
- BiologyThe Journal of Biological Chemistry
The cloning of a subunit 5-HT3B with ∼44% amino acid identity to 5-ht3A that specifically modified 5- HT3Areceptor kinetics, voltage dependence, and pharmacology is reported, suggesting that 5-TT3B might contribute to tissue-specific functional changes in 5-Hat3-mediated signaling and/or modulation.
The Multiplicity of Serotonin Receptors: Uselessly Diverse Molecules or an Embarrassment of Riches?
- Psychology, Biology
Evidence that is summarized in this review suggests that 5-HT receptors represent novel therapeutic targets for a number of neurologic and psychiatric diseases including migraine headaches, chronic pain conditions, schizophrenia, anxiety, depression, eating disorders, obsessive compulsive disorder, pervasive developmental disorders, and obesity-related conditions.