Sphingoid bases regulate the sigma-1 receptor—sphingosine and n,n’-dimethylsphingosine are endogenous agonists

HIGHLIGHTS

SUMMARY

Each protomer binding_site is supported and stabilized by beta sheets and four helices that constitute the bulk of the protein in the ER lumen. The identity of the ligand binding_site region from crystal_structures has generally confirmed previous biochemical analyses using covalent photoreactive radio-iodinated ligand probes of the native membrane-bound receptor. The S1R is shown with the cupin-like binding_site domain located in the ER lumen (center) and the N-terminal helix 1 bilayer imbedded (bottom right). Pathway 1 features mainly an aqueous entry involving the opening of a "lid" to expose the . . .

 



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