Chapter title |
Structural Perspectives on Sigma-1 Receptor Function
|
---|---|
Chapter number | 2 |
Book title |
Sigma Receptors: Their Role in Disease and as Therapeutic Targets
|
Published in |
Advances in experimental medicine and biology, March 2017
|
DOI | 10.1007/978-3-319-50174-1_2 |
Pubmed ID | |
Book ISBNs |
978-3-31-950172-7, 978-3-31-950174-1
|
Authors |
Assaf Alon, Hayden Schmidt, Sanduo Zheng, Andrew C. Kruse |
Editors |
Sylvia B. Smith, Tsung-Ping Su |
Abstract |
The sigma-1 receptor is an enigmatic ER-resident transmembrane protein linked to a variety of human diseases. Although the receptor was first cloned 20 years ago, the molecular structure of the protein and the mechanistic basis for its interaction with drug-like small molecules have remained unclear until recently. The determination of the first crystal structure of human sigma-1 offered the first detailed views of the sigma-1 architecture, and revealed an unusual overall fold with a single transmembrane helix in each protomer. The structure shows an overall trimeric receptor arrangement, and each protomer binds a single ligand molecule at the center of its carboxy-terminal domain. These results offer detailed molecular views of receptor structure, oligomerization, and ligand recognition, providing a framework for the next era of sigma-1 research. |
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Unknown | 1 | 50% |
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Mendeley readers
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Professor | 2 | 13% |
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Student > Ph. D. Student | 1 | 6% |
Researcher | 1 | 6% |
Other | 1 | 6% |
Unknown | 8 | 50% |
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Chemistry | 2 | 13% |
Pharmacology, Toxicology and Pharmaceutical Science | 1 | 6% |
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Unknown | 10 | 63% |