Biochemical studies on the sigma-1 receptor: a multidrug binding protein of enigmatic function
University of Wisconsin--Madison, 2008 - 220 pages
The sigma-1 receptor is an ubiquitously expressed transmembrane protein, notable for its ability to bind a variety of pharmacological agents. Although certain steroids bind to the sigma-1 receptor, a small endogenous molecule that regulates the activity of this receptor has not been identified. The sigma-1 receptor has been shown to have chaperone activity, modulate voltage gated ion channels, modulate Ca2+ release through the endoplasmic reticulum and promote the growth of cancer cells. The sigma-1 receptor does not display any homology to known mammalian proteins but shares homology with the steroid enzyme C8- C7 sterol isomerase from yeast.
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1 Photoprobes used in the identification of the sigma1 receptor
3 Pharmacophore for high affinity binding to the sigma1 receptor
4 Sequence Alignment of sigma1 receptor from different species
22 other sections not shown
1.4 K+ channel activity affinity column agonists amine amino acids amylose antagonists assay buffer containing C-terminal Ca2+ Chapter CHO-K1 cells cloning coli compounds concentration COS-7 cells D-erythro sphingosine detergent domain eluted endogenous expression extraction Factor Xa fenpropimorph Figure fusion protein guinea pig guinea pig liver guinea pig sigma-1 haloperidol high affinity hydrophobic incubated inhibition of 3H]-(+)-pentazocine inhibitor interaction ion channels IP3 receptor Kd values knockout mouse LDAO ligand binding lipid long alkyl chain MBP-sigma CT MBP-sigma-1 receptor fusion mediated modulation neurons Ni2+ overexpression pentazocine pentazocine binding Pharmacol photoaffinity labeling photolabeling pig liver membranes pig sigma-1 receptor plasmid polyclonal antibody pure sigma-1 receptor purification purified sigma-1 receptor receptor fusion protein Ruoho's laboratory showed sigma ligands sigma-1 receptor knockout sigma-1 receptor ligand SIPi receptor soluble specific sphingolipid sphingosine kinase sphingosine kinase-1 sphingosine-1 phosphate sterol structural transfected transmembrane tridemorph Triton western blotting wildtype