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σ1 RECEPTOR

σ1 Receptor ligand binding: an open-and-shut case

Nature Structural & Molecular Biologyvolume 25pages992993 (2018) | Download Citation

The σ1 receptor, an endoplasmic reticulum–resident transmembrane protein, modulates many physiological and pathological processes and binds multiple drugs, but is nonetheless poorly understood. In a recent issue, Kruse and colleagues illustrate structural differences between agonist- and antagonist-bound receptor and propose that agonist binding may impair oligomerization, making a major step in understanding σ1 function. They also use a combination of kinetic and molecular dynamic modeling to explain how ligands access the binding pocket.

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Acknowledgements

Supported by grants from the National Institute on Drug Abuse (DA07242 and DA06241), the Mayday Fund, and the McManus Charitable Trust to G.W.P.; a grant from the National Cancer Institute (CA08748) to SKI, MSKCC; and an American Cancer Society institutional research grant through the Sidney Kimmel Cancer Center at Thomas Jefferson University, a Drexel University Clinical and Translational Research Institute grant, and a Sidney Kimmel Cancer Center Consortium Pilot Study Award to F.J.K.

Author information

Affiliations

  1. Department of Cancer Biology, Thomas Jefferson University, Philadelphia, PA, USA

    • Felix J. Kim
  2. Sidney Kimmel Cancer Center at Thomas Jefferson University, Philadelphia, PA, USA

    • Felix J. Kim
  3. Department of Neurology and Molecular Pharmacology Program, Memorial Sloan Kettering Cancer Center, New York, NY, USA

    • Gavril W. Pasternak

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Competing interests

F.J.K. is a cofounder of Context Therapeutics.

Corresponding author

Correspondence to Gavril W. Pasternak.

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DOI

https://doi.org/10.1038/s41594-018-0146-1

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