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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...
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.
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...
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:

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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

Peptide receptor expression in GEP-NET.

Jean Claude Reubi1

  • 1Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, P.O. Box 62, Murtenstrasse 31, CH-3010, Berne, Switzerland. reubi@pathology.unibe.ch

Virchows Archiv : an International Journal of Pathology
|August 9, 2007
PubMed
Summary

Gastroenteropancreatic neuroendocrine tumors (GEP-NET) frequently express somatostatin receptors, enabling targeted therapies and diagnostics. These tumors also express other peptide receptors, opening avenues for multireceptor-based treatments.

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Area of Science:

  • Oncology
  • Endocrinology
  • Molecular Biology

Background:

  • Peptide receptors are increasingly found on human cancers.
  • Somatostatin receptors (sst) are highly expressed in gastroenteropancreatic neuroendocrine tumors (GEP-NET).
  • The sst(2) subtype is predominant in GEP-NET.

Purpose of the Study:

  • To review the role of peptide receptors in GEP-NET.
  • To highlight clinical applications of somatostatin receptor expression.
  • To explore potential for multireceptor targeting in GEP-NET.

Main Methods:

  • Literature review of peptide receptor expression in GEP-NET.
  • Analysis of somatostatin receptor subtypes and their clinical relevance.
  • Investigation of co-expression of other peptide receptors.

Main Results:

  • Somatostatin receptors, particularly sst(2), are key targets for GEP-NET therapy and diagnostics (e.g., Octreoscan, peptide receptor radiotherapy).
  • GEP-NET can express multiple peptide receptors, including glucagon-like peptide 1, secretin, cholecystokinin 2, bombesin, neuropeptide Y, and vasoactive intestinal peptide receptors.
  • Simultaneous expression of several peptide receptors offers opportunities for in vivo multireceptor targeting.

Conclusions:

  • Peptide receptor expression is a fundamental characteristic of GEP-NET.
  • Targeting somatostatin receptors is clinically established for GEP-NET.
  • Co-expression of multiple peptide receptors presents a promising strategy for advanced GEP-NET treatments.