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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
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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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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...
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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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GPCR Signaling: A Study of the Interplay Between Structure, Energy, and Function.

Yann Chalopin1

  • 1Structures, Properties and Modeling of Solids Laboratory Physics Department, CentraleSupélec/National Center for the Scientific Research, University of Paris-Saclay, Gif-sur-Yvette, France.

Proteins
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This study reveals how energy dissipation directs signaling in G protein-coupled receptors (GPCRs). Anisotropic vibrational energy flow creates pre-configured pathways for allosteric communication.

Keywords:
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Area of Science:

  • Biophysics
  • Structural Biology
  • Computational Biology

Background:

  • G protein-coupled receptors (GPCRs) are crucial for signal transduction but the mechanisms of allosteric communication remain incompletely understood.
  • Understanding how conformational changes propagate through GPCRs is vital for deciphering their function.

Purpose of the Study:

  • To investigate the role of energy dissipation in directing intramolecular signaling pathways within GPCRs.
  • To develop a physics-based framework for characterizing allosteric communication.

Main Methods:

  • Modeled protein residues as coupled oscillators to create a vibrational energy localization landscape.
  • Quantified directional energy flux between residues to identify signaling pathways.
  • Analyzed crystal structures of CB1 and CCR5 receptors.

Main Results:

  • Identified distinct pathways for energy and information transfer within GPCRs.
  • Revealed anisotropic patterns of energy dissipation that align with functional dynamics.
  • Demonstrated that these patterns represent pre-configured channels for allosteric signaling.

Conclusions:

  • Energy dissipation plays a critical role in directing allosteric communication in GPCRs.
  • The methodology provides a new approach to dissecting allosteric pathways.
  • Findings have implications for structure-based drug design targeting GPCRs.