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Updated: Jun 20, 2026

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Recent Advances in the Development of Sigma Receptor (Radio)Ligands and Their Application in Tumors

Tao Wang1,2,3, Na Sun1, Yanxi Ma1

  • 1Department of Nuclear Medicine, Xinqiao Hospital, Army Medical University, Chongqing 400037, China.

ACS Pharmacology & Translational Science
|April 17, 2025
PubMed

Insights

This review explores sigma-1 receptor (σ1R) and sigma-2 receptor (σ2R) ligands for cancer therapy and imaging. It details ligand development, tumor applications, and radiopharmaceutical innovations for improved cancer treatment.

Area of Science:

  • Oncology
  • Radiochemistry
  • Pharmacology

Background:

  • Cancer is a leading global cause of death with complex mechanisms.
  • Sigma-1 receptor (σ1R) is vital for tumor survival and migration.
  • Sigma-2 receptor (σ2R) is closely linked to tumor cell proliferation.

Purpose of the Study:

  • To review sigma-1 receptor (σ1R) and sigma-2 receptor (σ2R) roles in neoplasms.
  • To summarize ligand and radio-ligand development for tumor applications.
  • To discuss innovations in radiopharmaceuticals for cancer imaging and therapy.

Main Methods:

  • Comprehensive literature review on σ1R and σ2R ligands.
  • Classification of chemical structures and targeted ligand possibilities.
  • Analysis of chiral structures and pharmacokinetic properties of radiopharmaceuticals.

Main Results:

  • σ1R and σ2R are key targets in cancer research.
  • Development of various ligands and radio-ligands for diagnostic and therapeutic use.
  • Insights into structure-activity relationships for improved drug design.

Conclusions:

  • Ligands targeting σ1R and σ2R show promise in cancer treatment and imaging.
  • Dual/multitargeted ligands offer potential for enhanced efficacy.
  • Further development of radiopharmaceuticals can advance cancer care.

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