This Article Full Text Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Aydar, E. Articles by Djamgoz, M. B. A. Search for Related Content PubMed PubMed Citation Articles by Aydar, E. Articles by Djamgoz, M. B. A. Related Collections Cellular Pathobiology Cellular Pathobiology: Metabolism and Physiology

Sigma Receptors and Cancer

Possible Involvement of Ion Channels

Department of Biological Sciences, Sir Alexander Fleming Building, Imperial College, London, United Kingdom

The sigma () receptor and its agonists have been implicated in a myriad of cellular functions, biological processes and diseases. Whereas the precise molecular mechanism(s) of receptors and their involvement in cancer cell biology have not been elucidated, recent work has started to shed some light on these issues. A molecular model has been proposed for the cloned 1 receptor; the precise molecular nature of the 2 receptor remains unknown. receptors have been found to be frequently up-regulated in human cancer cells and tissues. 2 receptor drugs particularly have been shown to have antiproliferative effects. An interesting possibility is that and/or 1 drugs could produce anticancerous effects by modulating ion channels. As well as proliferation, a variety of other metastatic cellular behaviors such as adhesion, motility, and secretion may also be affected. Other mechanisms of receptor action may involve interaction with ankyrin and modulation of intracellular Ca²⁺ and sphingolipid levels. Although more research is needed to further define the molecular physiology of receptors, their involvement in the cellular pathophysiology of cancer raises the possibility that drugs could be useful as novel therapeutic agents.

This article has been cited by other articles:

				M. Johannessen, S. Ramachandran, L. Riemer, A. Ramos-Serrano, A. E. Ruoho, and M. B. Jackson Voltage-gated sodium channel modulation by {sigma}-receptors in cardiac myocytes and heterologous systems Am J Physiol Cell Physiol, May 1, 2009; 296(5): C1049 - C1057. [Abstract] [Full Text] [PDF]

				A. Pal, U. B. Chu, S. Ramachandran, D. Grawoig, L.-W. Guo, A. R. Hajipour, and A. E. Ruoho Juxtaposition of the Steroid Binding Domain-like I and II Regions Constitutes a Ligand Binding Site in the {sigma}-1 Receptor J. Biol. Chem., July 11, 2008; 283(28): 19646 - 19656. [Abstract] [Full Text] [PDF]

				C. P. Palmer, R. Mahen, E. Schnell, M. B.A. Djamgoz, and E. Aydar Sigma-1 Receptors Bind Cholesterol and Remodel Lipid Rafts in Breast Cancer Cell Lines Cancer Res., December 1, 2007; 67(23): 11166 - 11175. [Abstract] [Full Text] [PDF]

				J. Mei and G. W. Pasternak Modulation of Brainstem Opiate Analgesia in the Rat by {sigma}1 Receptors: A Microinjection Study J. Pharmacol. Exp. Ther., September 1, 2007; 322(3): 1278 - 1285. [Abstract] [Full Text] [PDF]

				C. Zeng, S. Vangveravong, J. Xu, K. C. Chang, R. S. Hotchkiss, K. T. Wheeler, D. Shen, Z.-P. Zhuang, H. F. Kung, and R. H. Mach Subcellular Localization of Sigma-2 Receptors in Breast Cancer Cells Using Two-Photon and Confocal Microscopy Cancer Res., July 15, 2007; 67(14): 6708 - 6716. [Abstract] [Full Text] [PDF]

				D. J. Rowland, Z. Tu, J. Xu, D. Ponde, R. H. Mach, and M. J. Welch Synthesis and In Vivo Evaluation of 2 High-Affinity 76Br-Labeled {sigma}2-Receptor Ligands J. Nucl. Med., June 1, 2006; 47(6): 1041 - 1048. [Abstract] [Full Text] [PDF]

				A. van Waarde, P. L. Jager, K. Ishiwata, R. A. Dierckx, and P. H. Elsinga Comparison of Sigma-Ligands and Metabolic PET Tracers for Differentiating Tumor from Inflammation J. Nucl. Med., January 1, 2006; 47(1): 150 - 154. [Abstract] [Full Text] [PDF]

				M. S. Ostenfeld, N. Fehrenbacher, M. Hoyer-Hansen, C. Thomsen, T. Farkas, and M. Jaattela Effective Tumor Cell Death by {sigma}-2 Receptor Ligand Siramesine Involves Lysosomal Leakage and Oxidative Stress Cancer Res., October 1, 2005; 65(19): 8975 - 8983. [Abstract] [Full Text] [PDF]

				A. Mukherjee, T. K. Prasad, N. M. Rao, and R. Banerjee Haloperidol-associated Stealth Liposomes: A POTENT CARRIER FOR DELIVERING GENES TO HUMAN BREAST CANCER CELLS J. Biol. Chem., April 22, 2005; 280(16): 15619 - 15627. [Abstract] [Full Text] [PDF]

				L. Wang, A. R. Prescott, B. A. Spruce, J. Sanderson, and G. Duncan Sigma Receptor Antagonists Inhibit Human Lens Cell Growth and Induce Pigmentation Invest. Ophthalmol. Vis. Sci., April 1, 2005; 46(4): 1403 - 1408. [Abstract] [Full Text] [PDF]