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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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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G-protein Coupled Receptors01:21

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G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
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Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization
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Structure-guided optimization of light-activated chimeric G-protein-coupled receptors.

Alexandra-Madelaine Tichy1, Wang Lok So1, Elliot J Gerrard2

  • 1Australian Regenerative Medicine Institute (ARMI), Faculty of Medicine, Nursing and Health Sciences, Monash University, 3800 Clayton/Melbourne, VIC, Australia; European Molecular Biology Laboratory Australia (EMBL Australia), Monash University, 3800 Clayton/Melbourne, VIC, Australia.

Structure (London, England : 1993)
|May 19, 2022
PubMed
Summary

Researchers optimized light-activated receptors by incorporating G-protein contacts, significantly enhancing signaling. This structure-guided approach enables new capabilities for targeted cell and network manipulation using engineered G-protein-coupled receptors (GPCRs).

Keywords:
G-protein-coupled receptorcell signalingoptogeneticsprotein engineering

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Area of Science:

  • Molecular Biology
  • Biochemistry
  • Structural Biology

Background:

  • G-protein-coupled receptors (GPCRs) are a vast human receptor family crucial for physiological processes.
  • GPCRs exhibit specific coupling to signaling pathways, a feature that can be tuned for novel receptor functions.
  • Recent high-resolution structures of GPCR-G-protein complexes offer opportunities for rational receptor engineering.

Purpose of the Study:

  • To demonstrate structure-guided optimization of light-activated OptoXRs.
  • To investigate the hypothesis that incorporating GPCR-Gα contacts improves receptor-G-protein coupling.
  • To develop a platform for engineering OptoXRs with enhanced signaling and spectral tuning for targeted manipulation.

Main Methods:

  • Evaluated structure-based alignments for chimeric receptor fusion.
  • Engineered a light-activated beta-2 adrenergic receptor (β₂AR) by incorporating GPCR-Gα contacts.
  • Assessed signaling function of engineered OptoXRs and performed spectral tuning.

Main Results:

  • Incorporating Gα contacts into a light-activated β₂AR increased signaling 7- to 20-fold compared to other designs.
  • Elimination of these contacts diminished receptor function, validating their importance.
  • The developed platform enabled optimization of another OptoXR and allowed for spectral tuning.

Conclusions:

  • Structure-guided engineering by incorporating GPCR-Gα contacts significantly enhances OptoXR signaling.
  • This approach provides a powerful platform for developing novel OptoXRs with tailored functions.
  • Optimized OptoXRs can be utilized for precise cell and network manipulation.