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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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Transducer Mechanism: Enzyme-Linked Receptors01:27

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Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
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GPCRs Regulate Adenylyl Cylase Activity01:09

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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 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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Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the...
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Related Experiment Video

Updated: Aug 6, 2025

Modified Yeast-Two-Hybrid System to Identify Proteins Interacting with the Growth Factor Progranulin
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Novel insight on GRP/GRPR axis in diseases.

Hao-Lu Sun1, Qiu-Ying Ma2, He-Ge Bian1

  • 1School of Basic Medical Sciences, Anhui Medical University, Anhui, China.

Biomedicine & Pharmacotherapy = Biomedecine & Pharmacotherapie
|March 18, 2023
PubMed
Summary

The gastrin-releasing peptide receptor (GRPR) and its ligand gastrin-releasing peptide (GRP) are implicated in numerous diseases, including inflammation, cardiovascular issues, neurological disorders, and cancer. Targeting the GRP/GRPR axis offers potential therapeutic strategies for various conditions.

Keywords:
CancersCardiovascular diseasesGRP/GRPR axisInflammation diseasesKidney diseasesNeurological diseases

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Area of Science:

  • Molecular Biology
  • Cellular Signaling
  • Disease Pathophysiology

Background:

  • The gastrin-releasing peptide receptor (GRPR), a G protein-coupled receptor (GPCR), binds gastrin-releasing peptide (GRP) and influences diverse biological functions.
  • GRP/GRPR signaling is implicated in the pathophysiology of inflammatory diseases, cardiovascular diseases, neurological disorders, and various cancers.
  • While GPCRs are drug targets, the specific roles of GRPR in disease progression require further exploration.

Purpose of the Study:

  • To review the pathophysiological roles of the GRP/GRPR signaling axis in various diseases.
  • To highlight the potential of the GRP/GRPR axis as a therapeutic target.
  • To summarize current research on GRP/GRPR involvement in disease.

Main Methods:

  • Literature review of existing research on GRP/GRPR signaling.
  • Analysis of GRP/GRPR involvement in immune, cardiovascular, neurological, and oncological pathways.
  • Examination of pro-gastrin-releasing peptide (ProGRP) as a potential tumor marker.

Main Results:

  • GRP/GRPR signaling is crucial in neutrophil chemotaxis and inflammation via pathways like PI3K, PKC, and MAPK.
  • GRP/GRPR activation in the cardiovascular system contributes to diseases like myocardial infarction through ICAM-1, VCAM-1, ERK1/2, MAPK, and AKT.
  • The GRP/GRPR axis is upregulated in lung, cervical, colorectal, renal cell, and head and neck cancers, with GRP acting as a mitogen.

Conclusions:

  • The GRP/GRPR axis plays significant roles in inflammation, cardiovascular disease, neurological function, and cancer development.
  • Pro-gastrin-releasing peptide (ProGRP) shows promise as an early diagnostic tumor marker.
  • Targeting the GRP/GRPR signaling pathway presents a promising therapeutic avenue for multiple diseases.