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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high affinity and are together...
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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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Class-B GPCR activation: is ligand helix-capping the key?

Jean-Michel Neumann1, Alain Couvineau, Samuel Murail

  • 1CEA, Institut de Biologie et Technologies de Saclay, URA CNRS 2096, Laboratoire des Protéines Membranaires, 91191Gif sur Yvette Cedex, France.

Trends in Biochemical Sciences
|June 17, 2008
PubMed
Summary

Researchers identified a common helix N-capping motif in class B G-protein-coupled receptors (GPCRs). This structural motif is key for receptor activation and may guide the development of new drugs targeting these essential proteins.

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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
14:02

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Published on: April 9, 2018

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Class B G-protein-coupled receptors (GPCRs) are crucial regulators of vital physiological processes.
  • They are activated by various peptide hormones, including secretin and glucagon.
  • Dysregulation of these receptors is implicated in numerous diseases.

Purpose of the Study:

  • To identify common structural features in class B GPCR-ligand N-terminal sequences.
  • To elucidate the role of these structural motifs in receptor activation.
  • To explore the potential for rational drug design targeting class B GPCRs.

Main Methods:

  • Sequence analysis of class B GPCR-ligand N-terminal regions.
  • Structural bioinformatics to identify conserved motifs.
  • Hypothesis generation regarding the mechanism of receptor activation.

Main Results:

  • Identification of a conserved helix N-capping motif present in all class B GPCR-ligand N-terminal sequences.
  • Proposal that this motif forms upon receptor binding, playing a key role in activation.
  • The motif's folded backbone conformation offers a template for drug design.

Conclusions:

  • The helix N-capping motif is a critical element for class B GPCR activation.
  • This finding provides a structural basis for understanding receptor-ligand interactions.
  • The identified motif can guide the rational design of therapeutics for diseases involving class B GPCRs.