Immunopharmacological profile of SR 31747: In vitro and in vivo studies on humoral and cellular responses

Casellas, Pierre; Bourrié, Bernard; Canat, Xavier; Carayon, Pierre; Buisson, Isabelle; Paul, Raymond; Brelière, Jean-Claude; Fur, G. Le

doi:10.1016/0165-5728(94)90113-9

Cited by 45 publications

(37 citation statements)

References 22 publications

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“…We have already established that SR 31747A affects a late event in the activation process of T lymphocytes which occurs during the S/G 2 /M phases of the cell cycle (14). This suggests that the function of SR-BP could be essential for T lymphocyte mitogenesis.…”

Section: Table II Inhibition Of [ 3 H]sr 31747a or [ 3 H](ϩ)-pentazocmentioning

confidence: 92%

“…7A) for membraneous SR-BP using We have shown previously (14) that SR 31747A is active at inhibiting lymphocyte proliferation while pentazocine is inactive. Since pentazocine does not block T lymphocyte proliferation while it prevents [ 3 H]SR 31747A binding, if SR 31747A is acting through SR-BP to block T lymphocyte mitogenesis, pentazocine should thereby prevent SR 31747A inhibition.…”

Section: Fig 5 Northern Blot Analysis Of Human Sr-bp Expressionmentioning

confidence: 97%

“…DISCUSSION SR 31747A is an immunomodulating agent eliciting high affinity for sigma receptors. It demonstrates immunosuppressive properties both in vitro and in vivo (14). This compound, which blocks the proliferation of lymphocytes at nanomolar concentrations, displays a spectrum of activity distinct from current immunosuppressive agents (35).…”

Section: Fig 5 Northern Blot Analysis Of Human Sr-bp Expressionmentioning

confidence: 99%

“…However, Liu et al (12), using a panel of sigma ligands, demonstrated a high correlation between drug binding potency at sigma sites and inhibition of splenocyte proliferation, suggesting that sigma receptors may function as immunoregulators. SR 31747A was first described by Paul et al (13) as a ligand able to compete with a very high potency with all known sigma ligands and to inhibit mitogen-induced mouse and human T cell proliferation with a potency similar to that of cyclosporin A (14). However, unlike cyclosporin A, SR 31747A does not alter early cellular events, but rather interferes at steps further along the pathway leading to proliferation, most probably during the S phase (14).…”

mentioning

confidence: 99%

“…SR 31747A was first described by Paul et al (13) as a ligand able to compete with a very high potency with all known sigma ligands and to inhibit mitogen-induced mouse and human T cell proliferation with a potency similar to that of cyclosporin A (14). However, unlike cyclosporin A, SR 31747A does not alter early cellular events, but rather interferes at steps further along the pathway leading to proliferation, most probably during the S phase (14). Multiple receptors have been described (8,(15)(16)(17)(18)(19).…”

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confidence: 99%

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Purification and Characterization of the Human SR 31747A-binding Protein

Jbilo

Vidal

Paul

et al. 1997

Journal of Biological Chemistry

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Section: Table II Inhibition Of [ 3 H]sr 31747a or [ 3 H](ϩ)-pentazocmentioning

confidence: 92%

Section: Fig 5 Northern Blot Analysis Of Human Sr-bp Expressionmentioning

confidence: 97%

Section: Fig 5 Northern Blot Analysis Of Human Sr-bp Expressionmentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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Purification and Characterization of the Human SR 31747A-binding Protein

Jbilo

Vidal

Paul

et al. 1997

Journal of Biological Chemistry

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Enhancement of endotoxin‐induced interleukin‐10 production by SR 31747A, a sigma ligand

et al. 1995

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SR 31747A is a new sigma ligand eliciting immunosuppressive and anti-inflammatory properties. Here, we show that SR 31747A greatly enhances lipopolysaccharide (LPS)-induced systemic release of interleukin (IL)-10, while it inhibits the secretion of tumor necrosis factor (TNF)-alpha and interferon (IFN)-gamma. In line with this finding, we also show by using quantitative reverse transcription-polymerase chain reaction analysis that SR 31747A increased LPS-induced IL-10 mRNA accumulation in spleen cells, whereas the level of both TNF-alpha and IFN-gamma mRNA was dramatically decreased. The enhancement of IL-10 production by SR 31747A treatment was also apparent in nude and severe-combined immunodeficient mice treated with LPS, clearly indicating that T and B cells were not involved. Finally, SR 31747A conferred protection against the lethal effect of LPS. The finding that SR 31747A strongly stimulates the synthesis of the natural anti-inflammatory cytokine IL-10, a property not observed with dexamethasone, provides new insights for the clinical use of this original compound, particularly in chronic inflammatory diseases where IL-10 is believed to be a pivotal regulatory component.

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Sigma1 Pharmacology in the Context of Cancer

Kim

Maher

2017

Handbook of Experimental Pharmacology

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Sigma1 (also known as sigma-1 receptor, Sig1R, σ1 receptor) is a unique pharmacologically regulated integral membrane chaperone or scaffolding protein. The majority of publications on the subject have focused on the neuropharmacology of Sigma1. However, a number of publications have also suggested a role for Sigma1 in cancer. Although there is currently no clinically used anti-cancer drug that targets Sigma1, a growing body of evidence supports the potential of Sigma1 ligands as therapeutic agents to treat cancer. In preclinical models, compounds with affinity for Sigma1 have been reported to inhibit cancer cell proliferation and survival, cell adhesion and migration, tumor growth, to alleviate cancer-associated pain, and to have immunomodulatory properties. This review will highlight that although the literature supports a role for Sigma1 in cancer, several fundamental questions regarding drug mechanism of action and the physiological relevance of aberrant SIGMAR1 transcript and Sigma1 protein expression in certain cancers remain unanswered or only partially answered. However, emerging lines of evidence suggest that Sigma1 is a component of the cancer cell support machinery, that it facilitates protein interaction networks, that it allosterically modulates the activity of its associated proteins, and that Sigma1 is a selectively multifunctional drug target.

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Immunopharmacological profile of SR 31747: In vitro and in vivo studies on humoral and cellular responses

Cited by 45 publications

References 22 publications

Purification and Characterization of the Human SR 31747A-binding Protein

Purification and Characterization of the Human SR 31747A-binding Protein

Enhancement of endotoxin‐induced interleukin‐10 production by SR 31747A, a sigma ligand

Sigma1 Pharmacology in the Context of Cancer

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