The Experts below are selected from a list of 315 Experts worldwide ranked by ideXlab platform
Irmgard Wiesenberg - One of the best experts on this subject based on the ideXlab platform.
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thiazolidine diones specific ligands of the nuclear receptor retinoid z receptor retinoid acid receptor related orphan receptor α with potent Antiarthritic activity
Journal of Biological Chemistry, 1996Co-Authors: Martin Missbach, Bruno Jagher, Ivo Sigg, Sepideh Nayeri, Carsten Carlberg, Irmgard WiesenbergAbstract:Abstract Rat adjuvant arthritis is a chronic T cell-dependent autoimmune disease with many similarities to rheumatoid arthritis. We have identified a class of thiazolidine diones with high potency in suppressing chronic inflammation and joint destruction in this experimental model. The lead compound CGP 52608 (1-(3-allyl-4-oxothiazolidine-2-ylidene)-4-methylthiosemicarbazone) exhibits Antiarthritic activity at daily oral doses between 0.01 and 1 mg/kg and was shown to specifically activate the retinoid Z receptor/retinoid acid receptor-related orphan receptor α (RZR/RORα) in low nanomolar concentrations. This receptor is a novel member of the superfamily of ligand-inducible transcription factors, and we have recently identified the pineal gland hormone melatonin as a natural ligand. Structure-activity relationship studies with 13 closely related analogues of CGP 52608 revealed a striking correlation between RZR/RORα activation and Antiarthritic activity. We therefore suggest that nuclear signaling via RZR/RORα is a key mechanism in mediating the Antiarthritic effects of these thiazolidine diones and may open a novel therapeutic approach for the treatment of rheumatoid arthritis and other autoimmune diseases. The existence of a nuclear melatonin receptor may lead to a better understanding of the immunomodulatory actions of melatonin.
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Thiazolidine Diones, Specific Ligands of the Nuclear Receptor Retinoid Z Receptor/Retinoid Acid Receptor-related Orphan Receptor α with Potent Antiarthritic Activity
Journal of Biological Chemistry, 1996Co-Authors: Martin Missbach, Bruno Jagher, Ivo Sigg, Sepideh Nayeri, Carsten Carlberg, Irmgard WiesenbergAbstract:Abstract Rat adjuvant arthritis is a chronic T cell-dependent autoimmune disease with many similarities to rheumatoid arthritis. We have identified a class of thiazolidine diones with high potency in suppressing chronic inflammation and joint destruction in this experimental model. The lead compound CGP 52608 (1-(3-allyl-4-oxothiazolidine-2-ylidene)-4-methylthiosemicarbazone) exhibits Antiarthritic activity at daily oral doses between 0.01 and 1 mg/kg and was shown to specifically activate the retinoid Z receptor/retinoid acid receptor-related orphan receptor α (RZR/RORα) in low nanomolar concentrations. This receptor is a novel member of the superfamily of ligand-inducible transcription factors, and we have recently identified the pineal gland hormone melatonin as a natural ligand. Structure-activity relationship studies with 13 closely related analogues of CGP 52608 revealed a striking correlation between RZR/RORα activation and Antiarthritic activity. We therefore suggest that nuclear signaling via RZR/RORα is a key mechanism in mediating the Antiarthritic effects of these thiazolidine diones and may open a novel therapeutic approach for the treatment of rheumatoid arthritis and other autoimmune diseases. The existence of a nuclear melatonin receptor may lead to a better understanding of the immunomodulatory actions of melatonin.
Martin Missbach - One of the best experts on this subject based on the ideXlab platform.
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thiazolidine diones specific ligands of the nuclear receptor retinoid z receptor retinoid acid receptor related orphan receptor α with potent Antiarthritic activity
Journal of Biological Chemistry, 1996Co-Authors: Martin Missbach, Bruno Jagher, Ivo Sigg, Sepideh Nayeri, Carsten Carlberg, Irmgard WiesenbergAbstract:Abstract Rat adjuvant arthritis is a chronic T cell-dependent autoimmune disease with many similarities to rheumatoid arthritis. We have identified a class of thiazolidine diones with high potency in suppressing chronic inflammation and joint destruction in this experimental model. The lead compound CGP 52608 (1-(3-allyl-4-oxothiazolidine-2-ylidene)-4-methylthiosemicarbazone) exhibits Antiarthritic activity at daily oral doses between 0.01 and 1 mg/kg and was shown to specifically activate the retinoid Z receptor/retinoid acid receptor-related orphan receptor α (RZR/RORα) in low nanomolar concentrations. This receptor is a novel member of the superfamily of ligand-inducible transcription factors, and we have recently identified the pineal gland hormone melatonin as a natural ligand. Structure-activity relationship studies with 13 closely related analogues of CGP 52608 revealed a striking correlation between RZR/RORα activation and Antiarthritic activity. We therefore suggest that nuclear signaling via RZR/RORα is a key mechanism in mediating the Antiarthritic effects of these thiazolidine diones and may open a novel therapeutic approach for the treatment of rheumatoid arthritis and other autoimmune diseases. The existence of a nuclear melatonin receptor may lead to a better understanding of the immunomodulatory actions of melatonin.
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Thiazolidine Diones, Specific Ligands of the Nuclear Receptor Retinoid Z Receptor/Retinoid Acid Receptor-related Orphan Receptor α with Potent Antiarthritic Activity
Journal of Biological Chemistry, 1996Co-Authors: Martin Missbach, Bruno Jagher, Ivo Sigg, Sepideh Nayeri, Carsten Carlberg, Irmgard WiesenbergAbstract:Abstract Rat adjuvant arthritis is a chronic T cell-dependent autoimmune disease with many similarities to rheumatoid arthritis. We have identified a class of thiazolidine diones with high potency in suppressing chronic inflammation and joint destruction in this experimental model. The lead compound CGP 52608 (1-(3-allyl-4-oxothiazolidine-2-ylidene)-4-methylthiosemicarbazone) exhibits Antiarthritic activity at daily oral doses between 0.01 and 1 mg/kg and was shown to specifically activate the retinoid Z receptor/retinoid acid receptor-related orphan receptor α (RZR/RORα) in low nanomolar concentrations. This receptor is a novel member of the superfamily of ligand-inducible transcription factors, and we have recently identified the pineal gland hormone melatonin as a natural ligand. Structure-activity relationship studies with 13 closely related analogues of CGP 52608 revealed a striking correlation between RZR/RORα activation and Antiarthritic activity. We therefore suggest that nuclear signaling via RZR/RORα is a key mechanism in mediating the Antiarthritic effects of these thiazolidine diones and may open a novel therapeutic approach for the treatment of rheumatoid arthritis and other autoimmune diseases. The existence of a nuclear melatonin receptor may lead to a better understanding of the immunomodulatory actions of melatonin.
Salvatore Ragusa - One of the best experts on this subject based on the ideXlab platform.
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Analgesic and antiinflammatory activity in acute and chronic conditions of Trema guineense (Schum. et Thonn.) Ficalho and Trema micrantha Blume extracts in rodents
Phytotherapy Research, 1992Co-Authors: R. Barbera, A. Trovato, A. Rapisarda, Salvatore RagusaAbstract:The analgesic activity of extracts of Trema guineense (Schum. et Thonn.) Ficalho and Trema micranthan Blume were evaluated in mice by the acetic acid induced wirthing test and in rats by the hot plate method. The antiflammatory and Antiarthritic activities were evaluated in rats by the carrageenin-induced Oedema assay and Newbould's adjuvant arthritis test. Pharmacological activities were compared with indomethacin. The ether and ethanol extracts of both species showed a significant analgesic activity in both tests. As regards the antiinflammatory and antiinflammatory and Antiarthritic activities, the ether extract of Trema micrantha (1 kg of dry leaves) produced the highest percentage of inhibityion of carrageenin-induced oedema and adjuvant arthritis and this effect was comparable to that of indomethancin
Bruno Jagher - One of the best experts on this subject based on the ideXlab platform.
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thiazolidine diones specific ligands of the nuclear receptor retinoid z receptor retinoid acid receptor related orphan receptor α with potent Antiarthritic activity
Journal of Biological Chemistry, 1996Co-Authors: Martin Missbach, Bruno Jagher, Ivo Sigg, Sepideh Nayeri, Carsten Carlberg, Irmgard WiesenbergAbstract:Abstract Rat adjuvant arthritis is a chronic T cell-dependent autoimmune disease with many similarities to rheumatoid arthritis. We have identified a class of thiazolidine diones with high potency in suppressing chronic inflammation and joint destruction in this experimental model. The lead compound CGP 52608 (1-(3-allyl-4-oxothiazolidine-2-ylidene)-4-methylthiosemicarbazone) exhibits Antiarthritic activity at daily oral doses between 0.01 and 1 mg/kg and was shown to specifically activate the retinoid Z receptor/retinoid acid receptor-related orphan receptor α (RZR/RORα) in low nanomolar concentrations. This receptor is a novel member of the superfamily of ligand-inducible transcription factors, and we have recently identified the pineal gland hormone melatonin as a natural ligand. Structure-activity relationship studies with 13 closely related analogues of CGP 52608 revealed a striking correlation between RZR/RORα activation and Antiarthritic activity. We therefore suggest that nuclear signaling via RZR/RORα is a key mechanism in mediating the Antiarthritic effects of these thiazolidine diones and may open a novel therapeutic approach for the treatment of rheumatoid arthritis and other autoimmune diseases. The existence of a nuclear melatonin receptor may lead to a better understanding of the immunomodulatory actions of melatonin.
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Thiazolidine Diones, Specific Ligands of the Nuclear Receptor Retinoid Z Receptor/Retinoid Acid Receptor-related Orphan Receptor α with Potent Antiarthritic Activity
Journal of Biological Chemistry, 1996Co-Authors: Martin Missbach, Bruno Jagher, Ivo Sigg, Sepideh Nayeri, Carsten Carlberg, Irmgard WiesenbergAbstract:Abstract Rat adjuvant arthritis is a chronic T cell-dependent autoimmune disease with many similarities to rheumatoid arthritis. We have identified a class of thiazolidine diones with high potency in suppressing chronic inflammation and joint destruction in this experimental model. The lead compound CGP 52608 (1-(3-allyl-4-oxothiazolidine-2-ylidene)-4-methylthiosemicarbazone) exhibits Antiarthritic activity at daily oral doses between 0.01 and 1 mg/kg and was shown to specifically activate the retinoid Z receptor/retinoid acid receptor-related orphan receptor α (RZR/RORα) in low nanomolar concentrations. This receptor is a novel member of the superfamily of ligand-inducible transcription factors, and we have recently identified the pineal gland hormone melatonin as a natural ligand. Structure-activity relationship studies with 13 closely related analogues of CGP 52608 revealed a striking correlation between RZR/RORα activation and Antiarthritic activity. We therefore suggest that nuclear signaling via RZR/RORα is a key mechanism in mediating the Antiarthritic effects of these thiazolidine diones and may open a novel therapeutic approach for the treatment of rheumatoid arthritis and other autoimmune diseases. The existence of a nuclear melatonin receptor may lead to a better understanding of the immunomodulatory actions of melatonin.
Carsten Carlberg - One of the best experts on this subject based on the ideXlab platform.
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thiazolidine diones specific ligands of the nuclear receptor retinoid z receptor retinoid acid receptor related orphan receptor α with potent Antiarthritic activity
Journal of Biological Chemistry, 1996Co-Authors: Martin Missbach, Bruno Jagher, Ivo Sigg, Sepideh Nayeri, Carsten Carlberg, Irmgard WiesenbergAbstract:Abstract Rat adjuvant arthritis is a chronic T cell-dependent autoimmune disease with many similarities to rheumatoid arthritis. We have identified a class of thiazolidine diones with high potency in suppressing chronic inflammation and joint destruction in this experimental model. The lead compound CGP 52608 (1-(3-allyl-4-oxothiazolidine-2-ylidene)-4-methylthiosemicarbazone) exhibits Antiarthritic activity at daily oral doses between 0.01 and 1 mg/kg and was shown to specifically activate the retinoid Z receptor/retinoid acid receptor-related orphan receptor α (RZR/RORα) in low nanomolar concentrations. This receptor is a novel member of the superfamily of ligand-inducible transcription factors, and we have recently identified the pineal gland hormone melatonin as a natural ligand. Structure-activity relationship studies with 13 closely related analogues of CGP 52608 revealed a striking correlation between RZR/RORα activation and Antiarthritic activity. We therefore suggest that nuclear signaling via RZR/RORα is a key mechanism in mediating the Antiarthritic effects of these thiazolidine diones and may open a novel therapeutic approach for the treatment of rheumatoid arthritis and other autoimmune diseases. The existence of a nuclear melatonin receptor may lead to a better understanding of the immunomodulatory actions of melatonin.
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Thiazolidine Diones, Specific Ligands of the Nuclear Receptor Retinoid Z Receptor/Retinoid Acid Receptor-related Orphan Receptor α with Potent Antiarthritic Activity
Journal of Biological Chemistry, 1996Co-Authors: Martin Missbach, Bruno Jagher, Ivo Sigg, Sepideh Nayeri, Carsten Carlberg, Irmgard WiesenbergAbstract:Abstract Rat adjuvant arthritis is a chronic T cell-dependent autoimmune disease with many similarities to rheumatoid arthritis. We have identified a class of thiazolidine diones with high potency in suppressing chronic inflammation and joint destruction in this experimental model. The lead compound CGP 52608 (1-(3-allyl-4-oxothiazolidine-2-ylidene)-4-methylthiosemicarbazone) exhibits Antiarthritic activity at daily oral doses between 0.01 and 1 mg/kg and was shown to specifically activate the retinoid Z receptor/retinoid acid receptor-related orphan receptor α (RZR/RORα) in low nanomolar concentrations. This receptor is a novel member of the superfamily of ligand-inducible transcription factors, and we have recently identified the pineal gland hormone melatonin as a natural ligand. Structure-activity relationship studies with 13 closely related analogues of CGP 52608 revealed a striking correlation between RZR/RORα activation and Antiarthritic activity. We therefore suggest that nuclear signaling via RZR/RORα is a key mechanism in mediating the Antiarthritic effects of these thiazolidine diones and may open a novel therapeutic approach for the treatment of rheumatoid arthritis and other autoimmune diseases. The existence of a nuclear melatonin receptor may lead to a better understanding of the immunomodulatory actions of melatonin.