The Evolution of the Sigma-2 (σ2) Receptor from Obscure Binding Site to Bona Fide Therapeutic Target.
The sigma-2 (σ2) receptor represents one of the most poorly understood proteins in cell biology. Although this receptor was identified through in vitro binding studies over 25 years ago, the molecular identity of this protein is currently not unambiguously known, and the results from recent attempts to identify the σ2receptor through protein purification and mass spectral analysis have been the subject of debate in the literature. However, there is overwhelming data demonstrating that the σ2receptor is an important biomarker of tumor cell proliferation . The observation that σ2receptor agonists are potent anticancer agents whereas σ2antagonists block Aβ1-42 oligomer synaptic dysfunction in transgenic mouse models of Alzheimer's disease have clearly identified this protein as an important therapeutic target for the treatment of a variety of pathological conditions.
Department of Radiology, University of Pennsylvania, Philadelphia, PA, 19104, USA.
Chenbo
C
Zeng
Department of Radiology, University of Pennsylvania, Philadelphia, PA, 19104, USA.
Robert H
RH
Mach
D000544:Alzheimer Disease / Q000188:drug therapy / Q000378:metabolism; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use; D001665:Binding Sites / Q000502:physiology*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D017480:Receptors, sigma / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000970:Antineoplastic Agents; D017480:Receptors, sigma; C106107:sigma-2 receptor
Agonists; Antagonists; Cancer chemotherapy; Cell proliferation; σ2 receptors