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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.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
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G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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GPCR Desensitization01:12

GPCR Desensitization

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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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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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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.
GPCRs are also called heptahelical,...
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Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

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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.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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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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Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
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Emerging structural insights into biased GPCR signaling.

Arun K Shukla1, Garima Singh1, Eshan Ghosh1

  • 1Department of Biological Sciences and Bioengineering, Indian Institute of Technology, Kanpur 208016, India.

Trends in Biochemical Sciences
|December 3, 2014
PubMed
Summary
This summary is machine-generated.

Biased signaling in G protein-coupled receptors (GPCRs) offers new therapeutic avenues. Understanding ligand-receptor interactions and conformational changes is key to developing novel drugs for various diseases.

Keywords:
G protein-coupled receptors (GPCRs)biased agonismbiased signalingβ-arrestinβ2 adrenergic receptor’

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Area of Science:

  • Pharmacology
  • Molecular Biology
  • Biophysics

Background:

  • G protein-coupled receptors (GPCRs) are crucial cell surface receptors and major drug targets.
  • Classical pharmacology concepts are being redefined by biased GPCR signaling.
  • Biased signaling reveals extensive signaling diversity within the GPCR system.

Purpose of the Study:

  • To highlight recent advances in understanding biased GPCR signaling.
  • To provide mechanistic insights into ligand-receptor interactions and receptor conformational changes.
  • To identify key areas for future investigation in GPCR-biased signaling.

Main Methods:

  • Biophysical techniques
  • Structural biology approaches
  • Analysis of ligand-receptor interactions
  • Investigation of receptor conformational dynamics

Main Results:

  • Recent biophysical and structural studies offer new mechanistic insights into biased GPCR signaling.
  • Ligand-receptor interactions and receptor conformational changes are central to biased signaling.
  • Biased signaling expands therapeutic possibilities for GPCR-targeted diseases.

Conclusions:

  • Biased GPCR signaling represents a paradigm shift in receptor pharmacology.
  • Further research is needed for a complete molecular understanding of GPCR-biased signaling.
  • This understanding can lead to the development of more effective therapeutics.