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| Content Provider | PubMed Central |
|---|---|
| Author | Chu, Uyen B. Ramachandran, Subramaniam Hajipour, Abdol R. Ruoho, Arnold E. |
| Abstract | The sigma-1 receptor is a ligand-regulated ER resident chaperone involved in the maintenance of cellular homeostasis. Coupling of the sigma-1 receptor with various ER and/or plasma membrane ion channels is associated with its ability to regulate the locomotor activity and cellular proliferation produced in response to sigma-1 receptor ligands. A number of endogenous small molecules bind to the sigma-1 receptor and have been shown to regulate its activity; these include progesterone, N,N-dimethyltryptamine, D-erythro-sphingosine, and/or other endogenous lipids. We previously reported the synthesis of long chain N-alkylamine derivatives and the characterization of the structural-activity relationship between chain length of N-alkylamine and affinities at the sigma-1 receptor. Here, we present data demonstrating the photo-incorporation of one of these N-alkylamine derivatives, 4-NPPC12, to the sigma-1 receptor. MALDI-TOF-TOF and tandem mass spectrometry showed that 4-NPPC12 photo-inserted at histidine 154 of the derivatized population of the sigma-1 receptor. Interestingly, light dependent photo-insertion of 4-NPPC12 resulted in an enhanced electrophoretic mobility of only 50% of the derivatized receptor molecules as assessed by SDS polyacrylamide gel electrophoresis. The proposed binding and reactivity of 4-NPPC12 evokes a ligand binding model for the sigma-1 receptor that likely involves a receptor dimer and/or oligomer. |
| Related Links | http://dx.doi.org/10.1021/bi301517u |
| Ending Page | 868 |
| Page Count | 10 |
| Starting Page | 859 |
| File Format | |
| ISSN | 00062960 |
| e-ISSN | 15204995 |
| Journal | Biochemistry |
| Issue Number | 5 |
| Volume Number | 52 |
| Language | English |
| Publisher Date | 2013-02-05 |
| Access Restriction | Open |
| Subject Keyword | Biochemistry Research in Higher Education |
| Content Type | Text |
| Resource Type | Article |
| Subject | Biochemistry |
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