A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.
TLDR
In this paper, a ternary complex model was used to fit the data with high accuracy under conditions where the ligand used is either a full or a partial agonist and where the system is altered by the addition of guanine nucleotide or after treatment with group-specific reagents.About:
This article is published in Journal of Biological Chemistry.The article was published on 1980-08-10 and is currently open access. It has received 1499 citations till now. The article focuses on the topics: Ternary complex & Agonist.read more
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Crystal structure of the β2 adrenergic receptor-Gs protein complex.
Søren G. F. Rasmussen,Brian T. DeVree,Yaozhong Zou,Andrew C. Kruse,Ka Young Chung,Tong Sun Kobilka,Foon Sun Thian,Pil Seok Chae,Els Pardon,Els Pardon,Diane M. Calinski,Jesper Mosolff Mathiesen,Syed T. A. Shah,Joseph A. Lyons,Martin Caffrey,Samuel H. Gellman,Jan Steyaert,Jan Steyaert,Georgios Skiniotis,William I. Weis,Roger K. Sunahara,Brian K. Kobilka +21 more
TL;DR: This crystal structure represents the first high-resolution view of transmembrane signalling by a GPCR and the most surprising observation is a major displacement of the α-helical domain of Gαs relative to the Ras-like GTPase domain.
Journal ArticleDOI
The structure and function of G-protein-coupled receptors
TL;DR: G-protein-coupled receptors mediate most of the authors' physiological responses to hormones, neurotransmitters and environmental stimulants, and so have great potential as therapeutic targets for a broad spectrum of diseases.
Journal ArticleDOI
Transduction of receptor signals by beta-arrestins.
TL;DR: Another previously unappreciated strategy used by the receptors to regulate intracellular signaling pathways is indicated, which regulates aspects of cell motility, chemotaxis, apoptosis, and likely other cellular functions through a rapidly expanding list of signaling pathways.
Journal ArticleDOI
A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.
TL;DR: The experimental findings with the mutant receptor cannot be adequately rationalized within the theoretical framework of the Ternary Complex Model, and an extended version of this model that includes an explicit isomerization of the receptor to an active state closely models all the findings for both the mutant and the wild-type receptors.
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DREADDs for Neuroscientists.
TL;DR: A primer on DREADDs is provided highlighting key technical and conceptual considerations and identify challenges for chemogenetics going forward.
References
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Book
Applied Regression Analysis
Norman R. Draper,Harry Smith +1 more
TL;DR: In this article, the Straight Line Case is used to fit a straight line by least squares, and the Durbin-Watson Test is used for checking the straight line fit.
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A study of the desensitization produced by acetylcholine at the motor end-plate.
B. Katz,S. Thesleff +1 more
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Statistical Quality Control and Routine Data Processing for Radioimmunoassays and Immunoradiometric Assays
TL;DR: Numerous methods are available for the graphical display of radioimmunoassay dose—response curves, for curve-fitting and dose interpolation, for statistical quality control, and for automation and computerization of data processing.
Journal ArticleDOI
The glucagon-sensitive adenyl cyclase system in plasma membranes of rat liver. IV. Effects of guanylnucleotides on binding of 125I-glucagon.
TL;DR: In this article, the effects of nucleotides on binding of 125I-glucagon at specific binding sites in plasma membranes of rat liver GTP and GDP, equally and at a minimal concentration of 005 µm, stimulate the rate and degree of dissociation of bound labeled hormone, decrease uptake of glucagon by the membranes, and decrease the affinity of the binding sites for glucagon.
Journal ArticleDOI
Mathematical theory of complex ligand-binding systems at equilibrium: Some methods for parameter fitting
TL;DR: The equilibrium composition of a multicomponent crossreactive ligand-binding system is characterized by solving the mass action equations and several results in simulation and parameter fitting for radioimmunoassay, ion-protein reactions, etc., are derived from these equations.
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Crystal structure of the β2 adrenergic receptor-Gs protein complex.
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