scholarly journals A Slow Voltage-Dependent Na+-Current Induced by 5-Hydroxytryptamine and the G-Protein-Coupled Activation Mechanism in the Ganglion Cells of Aplysia.

1991 ◽  
Vol 41 (2) ◽  
pp. 259-275 ◽  
Author(s):  
Atsuko KUDO ◽  
Kazuhiko SASAKI ◽  
Yoshiaki TAMAZAWA ◽  
Mitsuhiko MATSUMOTO
Keyword(s):  
G Protein ◽  
Ganglion Cells ◽  
Activation Mechanism ◽  
Na Current ◽  
Voltage Dependent ◽  
G Protein Coupled

scholarly journals Molecular mechanisms of metabotropic GABAB receptor function

2021 ◽  
Vol 7 (22) ◽  
pp. eabg3362
Author(s):  
Hamidreza Shaye ◽  
Benjamin Stauch ◽  
Cornelius Gati ◽  
Vadim Cherezov
Keyword(s):  
G Protein ◽  
Molecular Mechanisms ◽  
Gabab Receptor ◽  
Neurological Diseases ◽  
Activation Mechanism ◽  
Allosteric Modulators ◽  
Inhibitory Neurotransmitter ◽  
Therapeutic Drugs ◽  
G Protein Coupled ◽  
The Brain

Metabotropic γ-aminobutyric acid G protein–coupled receptors (GABAB) represent one of the two main types of inhibitory neurotransmitter receptors in the brain. These receptors act both pre- and postsynaptically by modulating the transmission of neuronal signals and are involved in a range of neurological diseases, from alcohol addiction to epilepsy. A series of recent cryo-EM studies revealed critical details of the activation mechanism of GABAB. Structures are now available for the receptor bound to ligands with different modes of action, including antagonists, agonists, and positive allosteric modulators, and captured in different conformational states from the inactive apo to the fully active state bound to a G protein. These discoveries provide comprehensive insights into the activation of the GABAB receptor, which not only broaden our understanding of its structure, pharmacology, and physiological effects but also will ultimately facilitate the discovery of new therapeutic drugs and neuromodulators.

scholarly journals The mutational landscape of human olfactory G protein-coupled receptors

BMC Biology ◽  
2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Ramón Cierco Jimenez ◽  
Nil Casajuana-Martin ◽  
Adrián García-Recio ◽  
Lidia Alcántara ◽  
Leonardo Pardo ◽  
...  
Keyword(s):  
G Protein ◽  
Olfactory Receptors ◽  
Activation Mechanism ◽  
Gene Repertoire ◽  
Structural Level ◽  
Ongoing Research ◽  
Wide Range ◽  
Natural Variants ◽  
The Impact ◽  
G Protein Coupled

Abstract Background Olfactory receptors (ORs) constitute a large family of sensory proteins that enable us to recognize a wide range of chemical volatiles in the environment. By contrast to the extensive information about human olfactory thresholds for thousands of odorants, studies of the genetic influence on olfaction are limited to a few examples. To annotate on a broad scale the impact of mutations at the structural level, here we analyzed a compendium of 119,069 natural variants in human ORs collected from the public domain. Results OR mutations were categorized depending on their genomic and protein contexts, as well as their frequency of occurrence in several human populations. Functional interpretation of the natural changes was estimated from the increasing knowledge of the structure and function of the G protein-coupled receptor (GPCR) family, to which ORs belong. Our analysis reveals an extraordinary diversity of natural variations in the olfactory gene repertoire between individuals and populations, with a significant number of changes occurring at the structurally conserved regions. A particular attention is paid to mutations in positions linked to the conserved GPCR activation mechanism that could imply phenotypic variation in the olfactory perception. An interactive web application (hORMdb, Human Olfactory Receptor Mutation Database) was developed for the management and visualization of this mutational dataset. Conclusion We performed topological annotations and population analysis of natural variants of human olfactory receptors and provide an interactive application to explore human OR mutation data. We envisage that the utility of this information will increase as the amount of available pharmacological data for these receptors grow. This effort, together with ongoing research in the study of genetic changes in other sensory receptors could shape an emerging sensegenomics field of knowledge, which should be considered by food and cosmetic consumer product manufacturers for the benefit of the general population.

The Activation Mechanism of Class-III G-Protein Coupled Receptors

2004 ◽  
Vol 13 (1-2) ◽  
pp. 38-51
Author(s):  
J.-P. Pin ◽  
J. Kniazeff ◽  
C. Goudet ◽  
A.-S. Bessis ◽  
P. Rondard ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
Activation Mechanism ◽  
Class Iii ◽  
G Protein Coupled

scholarly journals The mutational landscape of human olfactory G protein-coupled receptors

2020 ◽  
Author(s):  
Ramón Cierco Jimenez ◽  
Nil Casajuana-Martin ◽  
Adrián García-Recio ◽  
Lidia Alcántara ◽  
Leonardo Pardo ◽  
...  
Keyword(s):  
G Protein ◽  
Web Application ◽  
Large Family ◽  
Activation Mechanism ◽  
Human Populations ◽  
Gene Repertoire ◽  
Functional Interpretation ◽  
Gpcr Activation ◽  
Wide Range ◽  
G Protein Coupled

ABSTRACTOlfactory receptors (ORs) constitute a large family of sensory proteins that enable us to recognize a wide range of chemical volatiles in the environment. By contrast to the extensive information about human olfactory thresholds for thousands of odorants, studies of the genetic influence on olfaction are limited to a few examples. Here, we analyzed a compendium of 118,057 natural variants in human ORs collected from the public domain. OR mutations were categorized depending on their genomic and protein contexts, as well as their frequency of occurrence in several human populations. Functional interpretation of the natural changes was estimated from the increasing knowledge of the structure and function of the G protein-coupled receptor (GPCR) family, to which ORs belong. Our analysis reveals an extraordinary diversity of natural variations in the olfactory gene repertoire between individuals and populations, with a significant number of changes occurring at structural conserved regions. A particular attention is paid to mutations in positions linked to the conserved GPCR activation mechanism that could imply phenotypic variation in the olfactory perception. An interactive web application (available at http://lmc.uab.cat/hORMdb) was developed for the management and visualization of this mutational dataset.

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