Potential Roles of G Protein-Coupled Receptor 30 (GPR30) in Migraine Pathophysiology

Yuning Yao1, Yang Gong1, Kegang Cao2

  • 1Department of Traditional Chinese Medicine, General Hospital of the PLA Northern Theater Command, Shenyang, Liaoning, People's Republic of China.

Insights

G protein-coupled receptor 30 (GPR30) plays a role in migraine pathogenesis, particularly in the trigeminal ganglion. Further research is needed to clarify its mechanisms and therapeutic potential for migraine treatment.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Migraine is a common neurological disorder with complex pathogenesis.
  • G protein-coupled receptor 30 (GPR30), initially viewed as a membrane estrogen receptor, is implicated in migraine pathophysiology.
  • GPR30 is notably expressed in the trigeminal ganglion, a key area in migraine.

Purpose of the Study:

  • To systematically review current research on GPR30's role in migraine pathogenesis.
  • To explore GPR30's molecular structure, ligands, distribution, and signaling pathways.
  • To assess GPR30's regulatory effects on migraine-associated neural functions.

Main Methods:

  • Systematic literature review of GPR30's involvement in neurological diseases, specifically migraine.
  • Analysis of studies on GPR30's molecular characteristics and distribution in the nervous system.
  • Evaluation of research on GPR30's impact on signal transduction pathways and neurovascular functions.

Main Results:

  • GPR30 influences migraine-related signal pathways and neural functions, but findings are sometimes contradictory.
  • Evidence linking GPR30 to estrogen-mediated regulation in migraine is inconclusive.
  • Clinical trials targeting GPR30 for migraine are lacking, and estrogen connections are not well-established.

Conclusions:

  • GPR30 presents a potential novel therapeutic target for migraine prevention and treatment.
  • Contradictory findings and lack of clinical data highlight challenges and future research directions.
  • Developing GPR30-targeted therapies requires further investigation into its precise mechanisms in migraine.

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...
13.9K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

2.4K
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.
90.7K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

5.7K
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,...
8.6K
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...
6.8K