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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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GPCR Desensitization01:12

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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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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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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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Transducer Mechanism: G Protein–Coupled Receptors01:30

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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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SnapShot: GPCR-Ligand Interactions.

Eshan Ghosh1, Kumari Nidhi1, Arun K Shukla1

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

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Summary
This summary is machine-generated.

G-protein-coupled receptors (GPCRs) are crucial for cellular signaling. Determined crystal structures reveal their inactive and active states, detailing ligand interactions and overall organization.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Structural Biology

Background:

  • G-protein-coupled receptors (GPCRs) are vital cell surface proteins that mediate cellular responses to external stimuli.
  • GPCRs function by transmitting signals across the plasma membrane, playing critical roles in numerous physiological processes.

Purpose of the Study:

  • To elucidate the structural basis of GPCR activation and ligand binding.
  • To provide atomic-level insights into the interactions between GPCRs and various ligands.

Main Methods:

  • X-ray crystallography was employed to determine the structures of GPCRs.
  • Receptor structures were resolved in both inactive and active conformations.
  • Analysis of complexes with chemically and functionally distinct ligands was performed.

Main Results:

  • High-resolution crystal structures of multiple GPCRs were obtained.
  • Structures captured receptors in distinct inactive and active conformational states.
  • Detailed atomic interactions between ligands and receptors were visualized.

Conclusions:

  • Crystal structures provide a comprehensive view of GPCR overall organization.
  • These structures offer unprecedented atomic detail on ligand-receptor binding mechanisms.
  • Understanding GPCR structures is key to deciphering cellular signaling pathways.