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Lecture

G Protein-Coupled Receptors: Signalling Diversity

In course

CH-411: Cellular signalling

Presentation of selected signalling pathways with emphasis on both the mechanism of action of the molecules involved, molecular interactions and the role of their spatio-temporal organization within the cell, considering cellular dimensions and conditions. ...

Description

This lecture delves into the intricate world of G protein-coupled receptors (GPCRs), focusing on their structure, activation, and signalling pathways. The slides cover topics such as the prominent class of 7TM receptors, ligand-induced bias effects, and the diverse responses triggered by different ligands. The lecture explores the activation of G proteins, the role of arrestin-mediated signals, and the implications of ligand bias on signalling pathways. It also discusses the internalisation of GPCRs and the functional oligomers formed by receptors. The presentation concludes with insights into the cellular localisation of GPCRs, including their activity within the cell and the potential signalling from endosomes.

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Instructor

Rudolf Hovius

Official source

Ontological neighbourhood

Biology

Cell biology: Cell signaling

Related concepts (32)

G protein-coupled receptor

G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses. They are coupled with G proteins.

G protein

G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell to its interior. Their activity is regulated by factors that control their ability to bind to and hydrolyze guanosine triphosphate (GTP) to guanosine diphosphate (GDP). When they are bound to GTP, they are 'on', and, when they are bound to GDP, they are 'off'. G proteins belong to the larger group of enzymes called GTPases.

Cell surface receptor

Cell surface receptors (membrane receptors, transmembrane receptors) are receptors that are embedded in the plasma membrane of cells. They act in cell signaling by receiving (binding to) extracellular molecules. They are specialized integral membrane proteins that allow communication between the cell and the extracellular space. The extracellular molecules may be hormones, neurotransmitters, cytokines, growth factors, cell adhesion molecules, or nutrients; they react with the receptor to induce changes in the metabolism and activity of a cell.

Signal transduction

Signal transduction is the process by which a chemical or physical signal is transmitted through a cell as a series of molecular events. Most commonly, protein phosphorylation is catalyzed by protein kinases, ultimately resulting in a cellular response. Proteins responsible for detecting stimuli are generally termed receptors, although in some cases the term sensor is used. The changes elicited by ligand binding (or signal sensing) in a receptor give rise to a biochemical cascade, which is a chain of biochemical events known as a signaling pathway.

Wnt signaling pathway

The Wnt signaling pathways are a group of signal transduction pathways which begin with proteins that pass signals into a cell through cell surface receptors. The name Wnt is a portmanteau created from the names Wingless and Int-1. Wnt signaling pathways use either nearby cell-cell communication (paracrine) or same-cell communication (autocrine). They are highly evolutionarily conserved in animals, which means they are similar across animal species from fruit flies to humans.

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