The σ_2 receptor: A novel protein for the imaging and treatment of cancer

摘要

The σ_2 receptor is an important target for the development of molecular probes in oncology because of its 10-fold higher density in proliferating tumor cells compared with that in quiescent tumor cells and because of the observation that σ_2 receptor agonists are able to kill tumor cells via apoptotic and nonapoptotic mechanisms. Although recent evidence indicates that the σ_2 receptor binding site is localized within the progesterone receptor membrane component 1 (PGRMC1), most information regarding this protein has been obtained using either radiolabeled or fluorescent receptor-based probes and from biochemical analysis of the effect of σ_2 selective ligands on cells grown in culture. This article reviews the development of σ_2 receptor ligands and presents an overview of how they have been used in vitro and in vivo to increase our understanding of the role of the σ_2 receptor in cancer and proliferation.