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Related Concept Videos

GPCR Desensitization01:12

GPCR Desensitization

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...
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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 cells.
Two...
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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.
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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.
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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, 7TM, or...

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Related Experiment Video

Updated: May 25, 2026

Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization
09:19

Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization

Published on: March 16, 2020

Ice breaking in GPCR structural biology.

Qiang Zhao1, Bei-li Wu

  • 1The Joint Laboratories of GPCR Research, Center of Structures and Functions of Drug Targets, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China. zhaoq@mail.shcnc.ac.cn

Acta Pharmacologica Sinica
|January 31, 2012
PubMed
Summary
This summary is machine-generated.

Solving high-resolution G-protein-coupled receptor (GPCR) structures remains challenging. Recent advances in expression, purification, and crystallization techniques are accelerating the determination of these crucial protein structures.

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Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization
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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
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Area of Science:

  • Structural biology
  • Biochemistry
  • Molecular biology

Background:

  • G-protein-coupled receptors (GPCRs) are a large superfamily of proteins with critical physiological roles.
  • Determining high-resolution GPCR structures is hindered by significant experimental challenges in protein expression, purification, and crystallization.
  • Despite these difficulties, recent breakthroughs have led to the elucidation of key GPCR structures, including CXCR4 and GPCR-G protein complexes.

Purpose of the Study:

  • To review the progress in expression, purification, and crystallization techniques for GPCRs.
  • To highlight technical advancements enabling GPCR structure determination.
  • To provide insights into future directions for GPCR structural studies.

Main Methods:

  • The study summarizes advancements in protein expression methodologies.
  • It reviews innovative purification strategies for membrane proteins like GPCRs.
  • The abstract discusses progress in crystallization techniques tailored for GPCRs.

Main Results:

  • There has been a notable increase in the number of solved GPCR structures.
  • High-impact structures, such as the peptide receptor CXCR4 and agonist-bound receptors, have been determined.
  • Progress is attributed to a combination of novel techniques, tools, and conceptual approaches.

Conclusions:

  • Recent technical innovations have significantly improved the ability to determine GPCR structures.
  • These advancements are crucial for understanding GPCR function and developing therapeutics.
  • Continued progress in expression, purification, and crystallization will facilitate future GPCR structural studies.