Related Experiment Video

Updated: Mar 29, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

17.5K

Molecular mechanisms of target recognition by lipid GPCRs: relevance for cancer

M T M van Jaarsveld1, J M Houthuijzen1, E E Voest1

  • 1Department of Molecular Oncology, the Netherlands Cancer Institute, Amsterdam, The Netherlands.

Oncogene
|December 8, 2015
PubMed

Insights

Lipid signaling through G-protein coupled receptors (GPCRs) is crucial in cancer. Understanding how these receptors interact with lipids offers new therapeutic targets for cancer treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Lipids play increasingly recognized roles in cancer metabolism, proliferation, metastasis, and chemotherapy resistance.
  • The precise mechanisms of lipid signal transduction in cancer remain incompletely understood.
  • G-protein coupled receptors (GPCRs) are frequently implicated in lipid signaling and represent potential therapeutic targets.

Purpose of the Study:

  • To explore the recognition of cancer-relevant lipids by GPCRs.
  • To compare the ligand-binding properties of over 50 lipid-binding receptors.
  • To examine the contribution of GPCR dysregulation to tumorigenesis and their therapeutic potential.

Main Methods:

  • Review and comparison of >50 lipid receptors and their ligand-binding properties.
  • Analysis of GPCR roles in cancer-related processes.
  • Discussion of therapeutic exploitation of lipid-targeting GPCRs.

Main Results:

  • GPCRs recognize four major classes of cancer-relevant lipids: lysophospholipids, phospholipids, fatty acids, and eicosanoids.
  • Dysregulation of these lipid receptors is linked to cancer development.
  • Significant potential exists for targeting these receptors therapeutically.

Conclusions:

  • GPCRs are key mediators of lipid signaling in cancer.
  • Targeting lipid-recognizing GPCRs presents a promising avenue for novel cancer therapies.
  • Further research into GPCR-lipid interactions can advance cancer treatment strategies.

More Related Videos

A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 406:56

A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4

Published on: March 10, 2018

14.6K
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

9.6K

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...
19.5K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

2.5K
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,...
7.7K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

7.0K
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.
134.1K
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...
8.3K