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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

GPCR Desensitization

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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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Chemotherapy-Induced Nausea and Vomiting: Cannabinoids01:21

Chemotherapy-Induced Nausea and Vomiting: Cannabinoids

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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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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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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 Receptors01:21

G-protein Coupled Receptors

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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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G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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Related Experiment Video

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Ex Vivo Release of Calcitonin Gene-Related Peptide from the Trigeminovascular System in Rodents
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GPR55 - a putative "type 3" cannabinoid receptor in inflammation.

Hyewon Yang, Juan Zhou, Christian Lehmann

    Journal of Basic and Clinical Physiology and Pharmacology
    |December 17, 2015
    PubMed
    Summary

    G protein-coupled receptor 55 (GPR55) is a novel cannabinoid receptor. Its unique signaling and distribution suggest therapeutic potential for inflammation.

    Area of Science:

    • Pharmacology
    • Neuroscience
    • Cellular Biology

    Background:

    • G protein-coupled receptor 55 (GPR55) interacts with cannabinoid ligands but differs from classical CB1 and CB2 receptors.
    • GPR55 exhibits low homology with CB1 and CB2 receptors, indicating a distinct receptor class.
    • The pharmacology and signaling pathways of GPR55 are not fully understood.

    Purpose of the Study:

    • To explore the unique characteristics of GPR55 as a potential "type 3" cannabinoid receptor.
    • To investigate the role of GPR55 in cellular processes and pathologies.
    • To evaluate GPR55 as a therapeutic target for inflammatory conditions.

    Main Methods:

    • Pharmacological characterization of GPR55.
    • Analysis of GPR55 signaling pathways.

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  • Investigation of GPR55 distribution in the central nervous system and peripheral tissues.
  • Exploration of GPR55-CB1 and GPR55-CB2 heteromerization.

    • Main Results:

    • GPR55 functions via a distinct signaling system and downstream cascade compared to CB1 and CB2 receptors.
    • Evidence suggests GPR55-CB1 and GPR55-CB2 heteromerization.
    • GPR55 is broadly distributed throughout the central nervous system and peripheral tissues.
    • GPR55 plays a role in various cellular processes and pathologies.

    Conclusions:

    • GPR55 represents a novel class of cannabinoid receptor, potentially a "type 3" receptor.
    • GPR55's unique signaling and broad distribution highlight its significance in physiological and pathological contexts.
    • GPR55 is a promising therapeutic target for inflammatory diseases.