Harnessing the genome for characterization of G-protein coupled receptors in cancer pathogenesis

Michael E Feigin1

  • 1Cold Spring Harbor Laboratory, NY, USA.

The FEBS Journal
|August 10, 2013
PubMed

Insights

G-protein coupled receptors (GPCRs) are increasingly recognized as crucial in cancer. This review highlights GPCRs as promising therapeutic targets for cancer treatment and personalized medicine.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • G-protein coupled receptors (GPCRs) are vital in physiological processes and drug development.
  • GPCRs can function as oncogenes or tumor suppressors by influencing cancer signaling networks.
  • Despite their known roles, GPCR-targeted drugs are underutilized in cancer therapy.

Purpose of the Study:

  • To review evidence supporting GPCRs as viable targets for cancer therapy.
  • To explore the role of GPCRs in cancer signaling, progression, and the tumor microenvironment.
  • To discuss the potential of GPCRs as therapeutic targets in personalized cancer medicine.

Main Methods:

  • Review of recent studies and large-scale genome-wide analyses of human tumors.
  • Analysis of GPCR alterations in cancer.
  • Evaluation of GPCRs' impact on cancer signaling pathways, tumor progression, invasion, metastasis, and the microenvironment.

Main Results:

  • Recent genomic analyses have identified novel GPCRs altered in various human cancers.
  • Evidence suggests GPCRs significantly influence cancer signaling pathways, tumor progression, invasion, and metastasis.
  • GPCRs play a role in modulating the tumor microenvironment.

Conclusions:

  • GPCRs are relevant and promising therapeutic targets for cancer treatment.
  • Genomic analysis is identifying specific GPCRs as targets for personalized cancer medicine.
  • Further research into GPCRs can lead to novel cancer therapies.

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...
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...
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, 7TM, or...
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.
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.
Cancer-Critical Genes I: Proto-oncogenes01:33

Cancer-Critical Genes I: Proto-oncogenes

Genes usually encode proteins necessary for the proper functioning of a healthy cell. Mutations can often cause changes to the gene expression pattern, thereby altering the phenotype.
When the function of certain critical genes, especially those involved in cell cycle regulation and cell growth signaling cascades, gets disrupted, it upsets the cell cycle progression. Such cells with unchecked cell cycles start proliferating uncontrollably and eventually develop into tumors.
Such genes that act...