Identification of sigma-2 receptor (sig-2R) has been controversial. Nevertheless, interest in sig-2R is high for its overexpression in tumors and potentials in oncology. Additionally, sig-2R antagonists inhibit Aβ binding at neurons, blocking the cognitive impairments of Alzheimer's disease. The most representative classes of sig-2R ligands are herein treated with focus on compounds that served to study sig-2R biology and to produce sig-2R: fluorescent ligands; multifunctional anticancer agents; and targeting nanoparticles. Although fluorescent ligands serve as 'green' pharmacological tools, sig-2R-multifunctional conjugates and sig-2R-targeted nanoparticles show how sig-2R targeting increases the activity of anticancer drugs in tumors with reduced toxicity. Altogether, this review draws a picture of the multiple approaches of sig-2R ligands in cancer therapy and as Alzheimer's disease modifying disease agents.
Keywords: multifunctional sigma-2 receptor ligands; sigma-2 receptor fluorescent ligands; sigma-2 receptor ligands; sigma-2 receptor targeted delivery; sigma-2 receptors.