Related Experiment Video

Updated: Dec 3, 2025

Extraction of Aqueous Metabolites from Cultured Adherent Cells for Metabolomic Analysis by Capillary Electrophoresis-Mass Spectrometry
11:39

Extraction of Aqueous Metabolites from Cultured Adherent Cells for Metabolomic Analysis by Capillary Electrophoresis-Mass Spectrometry

Published on: June 9, 2019

9.5K

Metabolite Sensing GPCRs: Promising Therapeutic Targets for Cancer Treatment?

Jesús Cosín-Roger1, Dolores Ortiz-Masia2, Maria Dolores Barrachina3

  • 1Hospital Dr. Peset, Fundación para la Investigación Sanitaria y Biomédica de la Comunitat Valenciana, FISABIO, 46017 Valencia, Spain.

Cells
|October 29, 2020
PubMed

Insights

Metabolite-activated G-protein-coupled receptors (GPCRs) regulate key cancer cell processes. Targeting these 19 specific GPCRs offers a promising new strategy for cancer therapy.

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • G-protein-coupled receptors (GPCRs) are the largest human receptor family, with ~800 members.
  • Metabolic alterations are hallmarks of cancer development.
  • Specific GPCRs are activated by metabolites, linking cellular metabolism to receptor signaling.

Purpose of the Study:

  • To review the functions of metabolite-sensing GPCRs.
  • To explore the potential of these GPCRs as pharmacological targets in cancer treatment.

Main Methods:

  • Literature review focusing on metabolite-sensing GPCRs and their roles in cancer.
  • Analysis of the functions and signaling pathways of 19 specific metabolite-sensing GPCRs.
  • Evaluation of the therapeutic potential of targeting these receptors in oncology.

Main Results:

  • Metabolite-sensing GPCRs regulate critical cancer cell processes including proliferation, differentiation, migration, and survival.
  • These receptors integrate metabolic signals to influence tumor progression.
  • The 19 identified GPCRs represent a focused group with significant implications for cancer biology.

Conclusions:

  • Metabolite-sensing GPCRs are crucial regulators of cancer cell behavior.
  • Targeting these specific GPCRs presents a viable and promising strategy for novel cancer therapies.
  • Further research into these targets could lead to significant advancements in cancer treatment.
Keywords:
G-protein-coupled receptorcancermetabolite sensing GPCR

More Related Videos

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators07:41

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

Published on: February 20, 2018

9.3K
Identification and Quantification of Deranged Metabolites in Critically Ill Patients Using NMR-Based Metabolomics11:02

Identification and Quantification of Deranged Metabolites in Critically Ill Patients Using NMR-Based Metabolomics

Published on: November 29, 2024

881

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...
15.4K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
8.2K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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.
Major types that are helpful drug targets include:
3.6K
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...
6.6K
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
7.5K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
5.7K