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Structural insights into G protein-coupled receptor signaling [PDF]

Structural Dynamics
G protein-coupled receptors (GPCRs) are the largest single family of transmembrane proteins encoded in the human genome, and they are among the most successful classes of therapeutic drug targets of all time.
Andrew Kruse
doaj   +2 more sources

High capacity in G protein-coupled receptor signaling [PDF]

Nature Communications, 2018
G protein-coupled receptors (GPCRs) activate intracellular signalling pathways upon extracellular stimulation. Here authors record single cell responses of GPCR signalling which allows the direct estimation of its channel capacity for each cell along ...
Amiran Keshelava, Gonzalo P. Solis, Micha Hersch, Alexey Koval, Mikhail Kryuchkov, Sven Bergmann, Vladimir L. Katanaev   +6 more
doaj   +4 more sources

The Open Question of How GPCRs Interact with GPCR Kinases (GRKs)

Biomolecules, 2021
G protein-coupled receptors (GPCRs), which regulate a vast number of eukaryotic processes, are desensitized by various mechanisms but, most importantly, by the GPCR kinases (GRKs).
M. Claire Cato, Yu-Chen Yen, Charnelle J. Francis, Kaely E. Elkins, Afzaal Shareef, Rachel Sterne-Marr, John J. G. Tesmer   +6 more
doaj   +1 more source

DEER Analysis of GPCR Conformational Heterogeneity

Biomolecules, 2021
G protein-coupled receptors (GPCRs) represent a large class of transmembrane helical proteins which are involved in numerous physiological signaling pathways and therefore represent crucial pharmacological targets.
Matthias Elgeti, Wayne L. Hubbell
doaj   +1 more source

G Protein-Coupled Receptor Kinases Take Central Stage

Cells, 2022
The relevance of the family of G protein-coupled receptor kinases (GRKs) is based on its key participation in the regulation and intracellular dynamics of the largest family of membrane receptors, namely G protein-coupled receptors (GPCRs) [...]
Federico Mayor, Cristina Murga
doaj   +1 more source

Quantitative approaches for studying G protein-coupled receptor signalling and pharmacology.

J Cell Sci
Pearce A, Redfern-Nichols T, Wills E, Rosa M, Manulak I, Sisk C, Huang X, Atakpa-Adaji P, Prole DL, Ladds G.   +9 more
europepmc   +2 more sources

Allosteric modulation of G protein-coupled receptor signaling

Frontiers in Endocrinology, 2023
G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins, regulate a wide array of physiological processes in response to extracellular signals. Although these receptors have proven to be the most successful class of drug targets,
Siyuan Shen, Chang Zhao, Chao Wu, Suyue Sun, Ziyan Li, Wei Yan, Zhenhua Shao   +6 more
doaj   +1 more source

Interaction of the Xanthine Nucleotide Binding Goα Mutant with G Protein-coupled Receptors [PDF]

, 1998
We constructed a double mutant version of the α subunit of Go that was regulated by xanthine nucleotides instead of guanine nucleotides (GoαX). We investigated the interaction between GoαX and G protein-coupled receptors in vitro.
Simon, Melvin I., Yu, Bo
core   +1 more source

Creation of photocyclic vertebrate rhodopsin by single amino acid substitution

eLife, 2022
Opsins are universal photoreceptive proteins in animals and can be classified into three types based on their photoreaction properties. Upon light irradiation, vertebrate rhodopsin forms a metastable active state, which cannot revert back to the original
Kazumi Sakai, Yoshinori Shichida, Yasushi Imamoto, Takahiro Yamashita   +3 more
doaj   +1 more source

Both Ligand- and Cell-Specific Parameters Control Ligand Agonism in a Kinetic Model of G Protein–Coupled Receptor Signaling [PDF]

, 2007
G protein–coupled receptors (GPCRs) exist in multiple dynamic states (e.g., ligand-bound, inactive, G protein–coupled) that influence G protein activation and ultimately response generation. In quantitative models of GPCR signaling that incorporate these
Kinzer-Ursem, Tamara L., Linderman, Jennifer J.   +1 more
core   +3 more sources