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Related Concept Videos

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 Receptors01:15

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...
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...

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Related Experiment Video

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Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
11:49

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

Orphan GPCR research.

S Chung1, T Funakoshi, O Civelli

  • 1Department of Pharmacology, University of California Irvine, Irvine, CA, USA.

British Journal of Pharmacology
|December 12, 2007
PubMed
Summary
This summary is machine-generated.

Orphan G protein-coupled receptors (GPCRs), initially lacking known ligands, are now being identified through reverse pharmacology and high-throughput screening. This review covers their history, deorphanization, and current challenges in ligand discovery.

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Neuroscience

Background:

  • Orphan G protein-coupled receptors (GPCRs) lack identified endogenous ligands.
  • They represent a significant area for drug discovery and understanding biological pathways.
  • Reverse pharmacology initially aimed to identify ligands for these receptors.

Purpose of the Study:

  • To review the historical progression of orphan GPCR research.
  • To detail the deorphanization of GPCRs and discovery of novel neuropeptides.
  • To discuss current challenges in identifying new GPCR ligands.

Main Methods:

  • Molecular biological analyses for initial GPCR identification.
  • Application of high-throughput screening in reverse pharmacology.
  • Literature review of historical discoveries and ongoing research.

Main Results:

  • Dozens of orphan GPCRs have been successfully deorphanized.
  • Novel neuropeptides have been discovered as endogenous ligands.
  • Significant challenges persist in the ongoing search for new ligands.

Conclusions:

  • The field of orphan GPCRs has evolved significantly from basic discovery to targeted ligand identification.
  • Technological advancements have accelerated deorphanization but new hurdles have emerged.
  • Continued research is crucial for fully understanding GPCR functions and therapeutic potential.