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The σ2 receptor: a novel protein for the imaging and treatment of cancer

Robert H Mach1, Chenbo Zeng, William G Hawkins

  • 1Mallinckrodt Institute of Radiology and ‡Department of Surgery, Washington University School of Medicine , St. Louis, Missouri 63110, United States.

Journal of Medicinal Chemistry
|June 6, 2013
PubMed

Insights

The sigma-2 (σ2) receptor, a target in oncology, is more abundant in tumor cells. Ligands targeting this receptor are crucial for understanding cancer and developing new therapies.

Area of Science:

  • Oncology
  • Molecular Pharmacology
  • Biochemistry

Background:

  • The sigma-2 (σ2) receptor is overexpressed in proliferating tumor cells, making it a promising target for cancer therapy.
  • σ2 receptor agonists induce tumor cell death through apoptotic and non-apoptotic pathways.
  • Recent studies suggest the σ2 receptor binding site is within the progesterone receptor membrane component 1 (PGRMC1).

Purpose of the Study:

  • To review the development of σ2 receptor ligands.
  • To provide an overview of how these ligands have advanced the understanding of the σ2 receptor's role in cancer.
  • To highlight the application of σ2 receptor ligands in both in vitro and in vivo cancer research.

Main Methods:

  • Review of existing literature on σ2 receptor ligand development.
  • Analysis of studies utilizing radiolabeled and fluorescent probes for σ2 receptor research.
  • Examination of biochemical analyses on the effects of σ2 selective ligands on cultured cells.

Main Results:

  • Development of various σ2 receptor ligands for molecular probing.
  • In vitro and in vivo studies demonstrate the utility of these ligands in cancer research.
  • Established the importance of σ2 receptor ligands in elucidating the receptor's function in cancer and proliferation.

Conclusions:

  • σ2 receptor ligands are essential tools for cancer research.
  • Further development and application of these ligands will enhance our understanding of cancer biology.
  • Targeting the σ2 receptor holds significant therapeutic potential in oncology.

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