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The Molecular Function of σ Receptors: Past, Present, and Future

Hayden R Schmidt¹, Andrew C Kruse¹

¹Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA.

Trends in Pharmacological Sciences

|August 8, 2019

Abstract:

The σ₁ and σ₂ receptors are enigmatic proteins that have attracted attention for decades due to the chemical diversity and therapeutic potential of their ligands. However, despite ongoing clinical trials with σ receptor ligands for multiple conditions, relatively little is known regarding the molecular function of these receptors. In this review, we revisit past research on σ receptors and discuss the interpretation of these data in light of recent developments. We provide a synthesis of emerging structural and genetic data on the σ₁ receptor and discuss the recent cloning of the σ₂ receptor. Finally, we discuss the major questions that remain in the study of σ receptors.

Keywords:

molecular pharmacology structural pharmacology σ(1) receptor σ(2) receptor/TMEM97

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