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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...
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...
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...
Dose-Response Relationship: Selectivity and Specificity01:25

Dose-Response Relationship: Selectivity and Specificity

Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and β2-adrenergic receptors...
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...

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Related Experiment Video

Updated: May 18, 2026

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

Opportunities for functional selectivity in GPCR antibodies.

David R Webb1, Tracy M Handel, Anke Kretz-Rommel

  • 1Department of Molecular Biology, The Scripps Research Institute, La Jolla, CA 92037, USA. dwebb@scripps.edu

Biochemical Pharmacology
|September 15, 2012
PubMed
Summary

Monoclonal antibodies (mAbs) are advancing G-protein-coupled receptor (GPCR) research and therapeutics. New insights into GPCRs enable the development of highly selective mAbs for novel treatments.

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Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Published on: April 9, 2018

Area of Science:

  • Pharmacology
  • Biophysics
  • Structural Biology

Background:

  • Monoclonal antibodies (mAbs) are established tools for studying receptor biology and pharmacology.
  • G-protein-coupled receptors (GPCRs) are increasingly targeted for therapeutic development, though less so than other targets.
  • Recent advances reveal GPCRs exist in multiple conformational states, regulated by ligands and proteins, enabling selective pathway activation.

Purpose of the Study:

  • To highlight the evolving understanding of G-protein-coupled receptor (GPCR) function.
  • To discuss the potential of monoclonal antibodies (mAbs) in targeting GPCRs.
  • To explore the development of novel therapeutics based on selective GPCR modulation.

Main Methods:

  • Review of recent pharmacological, structural, and biophysical data on GPCRs.
  • Analysis of new technologies for selecting mAbs against GPCRs.
  • Integration of GPCR conformational state information with mAb development strategies.

Main Results:

  • GPCRs are now understood to possess dynamic conformational states, not just "on" or "off" states.
  • Ligands and interacting proteins can finely tune GPCR structures, leading to selective signaling.
  • New mAb selection technologies facilitate targeting of specific GPCR conformational determinants.

Conclusions:

  • The detailed understanding of GPCRs' complex structures and functions opens avenues for highly selective mAb development.
  • Targeting specific GPCR conformational states with mAbs offers a promising strategy for novel therapeutic interventions.
  • The synergy between GPCR research and mAb technology is poised to drive innovation in drug discovery.