Expression of sigma 1 receptor in human breast cancer

Wang, B.; Rouzier, Roman; Albarracin, Constance T.; Şahin, Ayşe; Wagner, Peter J.; Yang, Yijun; Smith, Terry L.; Meric‐Bernstam, Funda; Aldaz, C. Marcelo; Hortobágyi, Gabriel N.; Pusztai, Lajos

doi:10.1007/s10549-004-8255-4

Cited by 14 publications

(20 citation statements)

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“…The role that j1 receptors play in cancer is not clear ( for review, see ref. 16), although it is frequently up-regulated in human cancer cells and tissues (7,16,17) and j receptors inhibit proliferation in carcinoma and melanoma cell lines, induce apoptosis in colon and mammary carcinoma cell lines, and reduce cellular adhesion in mammary carcinoma cell lines ( for review, see ref. 16).…”

Section: Introductionmentioning

confidence: 99%

Sigma-1 Receptors Bind Cholesterol and Remodel Lipid Rafts in Breast Cancer Cell Lines

et al. 2007

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Lipid rafts are membrane platforms that spatially organize molecules for specific signaling pathways that regulate various cellular functions. Cholesterol is critical for liquidordered raft formation by serving as a spacer between the hydrocarbon chains of sphingolipids, and alterations in the cholesterol contents of the plasma membrane causes disruption of rafts. The role that S receptors play in cancer is not clear, although it is frequently up-regulated in human cancer cells and tissues and S receptors inhibit proliferation in carcinoma and melanoma cell lines, induce apoptosis in colon and mammary carcinoma cell lines, and reduce cellular adhesion in mammary carcinoma cell lines. In this study, we provide molecular and functional evidence for the involvement of the enigmatic S1 receptors in lipid raft modeling by S1 receptor-mediated cholesterol alteration of lipid rafts in breast cancer cell lines. Cholesterol binds to cholesterol recognition domains in the COOH terminus of the S1 receptor. This binding is blocked by S receptor drugs because the cholesterol-binding domains form part of the S receptor drugbinding site, mutations of which abolish cholesterol binding. Furthermore, we outline a hypothetical functional model to explain the myriad of biological processes, including cancer, in which these mysterious receptors are involved. The findings of this study provide a biological basis for the potential therapeutic applications of lipid raft cholesterol regulation in cancer therapy using S receptor drugs. [Cancer Res 2007; 67(23):11166-75]

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Section: Introductionmentioning

confidence: 99%

Sigma-1 Receptors Bind Cholesterol and Remodel Lipid Rafts in Breast Cancer Cell Lines

et al. 2007

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“…The sigma-1 receptor is neuroprotective in stroke and cerebral ischemia (7), and has been linked to schizophrenia (8), Alzheimer disease (9), depression (10), and drug addiction (11). The receptor is up-regulated in tumors (12), and sigma-1 receptor agonists have been shown to inhibit neoplastic cell growth (13). The receptor also inhibits cell cycling in tumor cells, via K v 1.3 and Cl Ϫ channels (14,15), and it has been suggested that sigma-1 receptor antagonists may have chemotherapeutic properties (16).…”

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confidence: 99%

A Direct Interaction between the Sigma-1 Receptor and the hERG Voltage-gated K+ Channel Revealed by Atomic Force Microscopy and Homogeneous Time-resolved Fluorescence (HTRF®)

Balasuriya

D'Sa

Talker

et al. 2014

Journal of Biological Chemistry

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“…Immunocytochemistry of MCF-7 cells using an antibody made against a purified human sigma 1 receptor (Jbilo et al, 1997) revealed immunofluorescence only in MCF-7 cells transfected with human sigma 1 receptors, but not untransfected cells (Seth et al, 2001). Western blot analyses of proteins isolated from MCF-7 cells with antibodies made against peptide fragments of the human receptor revealed protein bands with no molecular weight reported (Wang et al, 2004), ~15-18 kDa (Mukherjee et al, 2005) or 25 kDa (Aydar et al, 2005). The former two studies utilized a commercially-available antibody that recognizes a peptide sequence between amino acids 50-100 (personal communication, Kent Williams, Santa Cruz Biotechnologies, Inc.).…”

Section: Discussionmentioning

confidence: 99%

An unambiguous assay for the cloned human sigma1 receptor reveals high affinity interactions with dopamine D4 receptor selective compounds and a distinct structure–affinity relationship for butyrophenones

Lee

Chen

Schetz

2008

European Journal of Pharmacology

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The ability of sigma 1 receptors to interact with a huge range of drug structural classes coupled with its wide distribution in the body has contributed to it being implicated as a possible therapeutic target for a broad array of disorders ranging from substance abuse to depression to Alzheimer's disease. Surprisingly, the reported affinity values for some sigma 1 receptor ligands vary more than 50-fold. The potential of the sigma 1 receptor as a pharmacotherapeutic target prompted us to develop an unambiguous assay system for measuring the affinity of ligands to the cloned human sigma 1 receptor. In the course of characterizing this system and determining the true affinity values for almost three dozen compounds, it was discovered that some dopamine D 4 receptor selective compounds bind sigma 1 receptors with high affinity. A systematic analysis of haloperidol-like compounds revealed a clear structure-affinity relationship amongst clinically relevant butyrophenones. The antidepressant fluvoxamine, the drug of abuse methamphetamine, and the neurosteroid progesterone were amongst the many ligands whose interactions with sigma 1 receptor were confirmed with our screening assay.

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Expression of sigma 1 receptor in human breast cancer

Cited by 14 publications

References 0 publications

Sigma-1 Receptors Bind Cholesterol and Remodel Lipid Rafts in Breast Cancer Cell Lines

Sigma-1 Receptors Bind Cholesterol and Remodel Lipid Rafts in Breast Cancer Cell Lines

A Direct Interaction between the Sigma-1 Receptor and the hERG Voltage-gated K+ Channel Revealed by Atomic Force Microscopy and Homogeneous Time-resolved Fluorescence (HTRF®)

An unambiguous assay for the cloned human sigma1 receptor reveals high affinity interactions with dopamine D4 receptor selective compounds and a distinct structure–affinity relationship for butyrophenones

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