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Sigma-2 receptor: past, present and perspectives on multiple therapeutic exploitations
Carmen Abate1, Mauro Niso1, Francesco Berardi1
1Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari ALDO MORO, Via Orabona 4, I-70125 Bari, Italy.
Future Medicinal Chemistry
|July 4, 2018
Summary
Sigma-2 receptor (sig-2R) ligands show promise in treating cancer and Alzheimer's disease. Research focuses on fluorescent ligands, anticancer agents, and nanoparticles for targeted therapy.
Area of Science:
- Pharmacology and Medicinal Chemistry
- Oncology
- Neuroscience
Background:
- The sigma-2 receptor (sig-2R) is overexpressed in tumors, indicating its potential in cancer therapy.
- Sig-2R antagonists may block Aβ binding in neurons, offering a therapeutic strategy for Alzheimer's disease.
Purpose of the Study:
- To review representative classes of sig-2R ligands.
- To highlight compounds used for studying sig-2R biology and therapeutic applications.
- To explore sig-2R's role in cancer and Alzheimer's disease.
Main Methods:
- Focus on fluorescent ligands as pharmacological tools.
- Examination of multifunctional anticancer agents conjugated with sig-2R targeting moieties.
- Analysis of sig-2R-targeted nanoparticles for drug delivery.
Main Results:
- Fluorescent ligands serve as valuable tools for sig-2R research.
- Sig-2R-multifunctional conjugates and targeted nanoparticles enhance anticancer drug efficacy in tumors.
- Targeted approaches reduce toxicity associated with anticancer therapies.
Conclusions:
- Sig-2R ligands offer diverse therapeutic strategies for cancer treatment.
- Targeting sig-2R presents a promising approach for modifying Alzheimer's disease progression.
- The review underscores the multifaceted potential of sig-2R ligands in medicine.
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