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Related Concept Videos

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...
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...
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...
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...
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids01:21

Chemotherapy-Induced Nausea and Vomiting: Cannabinoids

Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
Two synthetic agonists of THC,...

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BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
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BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells

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Off-target cannabinoid effects mediated by GPR55.

Christopher M Henstridge1

  • 1Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest, Hungary.

Pharmacology
|March 22, 2012
PubMed
Summary
This summary is machine-generated.

The orphan G-protein coupled receptor 55 (GPR55) is a novel target within the endocannabinoid system. Despite a complex cannabinoid profile, GPR55 shows therapeutic potential in cancer, bone health, and pain management.

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Area of Science:

  • Pharmacology
  • Endocrinology
  • Cell Biology

Background:

  • The endocannabinoid system offers significant therapeutic opportunities.
  • The orphan G-protein coupled receptor 55 (GPR55) emerged as a potential cannabinoid target.
  • GPR55 is expressed in various tissues and influences physiological and pathological processes.

Purpose of the Study:

  • To review GPR55 expression data.
  • To explore the therapeutic potential of GPR55.
  • To discuss the exploitation of GPR55 for medical applications.

Main Methods:

  • Literature review of GPR55 expression studies.
  • Analysis of GPR55's role in physiological and pathological contexts.
  • Speculation on therapeutic strategies targeting GPR55.

Main Results:

  • GPR55 is widely expressed across different cell types and tissues.
  • GPR55 participates in crucial biological functions, including cancer progression, bone resorption, and analgesia.
  • A definitive cannabinoid ligand profile for GPR55 remains elusive, complicating its classification.

Conclusions:

  • GPR55 represents a promising, albeit complex, therapeutic target.
  • Further research into GPR55 modulation could yield novel treatments for various conditions.
  • Targeting GPR55 offers potential for managing cancer, bone diseases, and pain.