Carcinostatic activity of a thiazolidinonylidene-hydrazonothiazolidinone derivative against DMBA-induced mammary carcinomata in female Sprague-Dawley rats

Schmidt-Ruppin, K. H.; Meisels, A; Schott, E.; Storni, A.; Schieweck, K.

doi:10.1007/bf01946310

Cited by 5 publications

(3 citation statements)

References 1 publication

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“…During the search for novel immunomodulating compounds, we discovered thiazolidine diones (TDs) 1 with potent antiarthritic activity in rat adjuvant arthritis. This chronic T cell-dependent autoimmune disease has many similarities to rheumatoid arthritis such as progressive joint destruction, enhanced T cell responses (Th1), and pronounced cytokine-mediated acutephase reactions (1)(2)(3)(4)(5)(6)(7). It was known that these TDs inhibit the growth of various experimental tumors.…”

Section: Rat Adjuvant Arthritis Is a Chronic T Cell-dependent Autoimmmentioning

confidence: 99%

Thiazolidine Diones, Specific Ligands of the Nuclear Receptor Retinoid Z Receptor/Retinoid Acid Receptor-related Orphan Receptor α with Potent Antiarthritic Activity

Missbach

Jagher

Sigg

et al. 1996

Journal of Biological Chemistry

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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 alpha (RZR/RORalpha) 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/RORalpha activation and antiarthritic activity. We therefore suggest that nuclear signaling via RZR/RORalpha 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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Section: Rat Adjuvant Arthritis Is a Chronic T Cell-dependent Autoimmmentioning

confidence: 99%

Thiazolidine Diones, Specific Ligands of the Nuclear Receptor Retinoid Z Receptor/Retinoid Acid Receptor-related Orphan Receptor α with Potent Antiarthritic Activity

Missbach

Jagher

Sigg

et al. 1996

Journal of Biological Chemistry

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“…A reduced food intake and a transient loss of weight were observed in treated rats and dogs. After the cessation of treatment, the animals regained weight and grew steadily throughout the remaining period of observation [3], The same was found in rats with DMBA-induced mam mary carcinomas [1,2]. About 30% of human breast cancers and almost 90% of chemically induced mammary cancers in rats are hormonedependent, and regress in response to endocrine therapy (ovariectomy, adrenalectomy and hypophysectomy).…”

Section: Gp 48 989 5-mcthyl-3-(2-methylallyl)-2-[(3-mcthyl-4-oxo-2-thmentioning

confidence: 81%

“…Ltd., Basle, Switzerland) is active against some induced and transplantable carcinomas in mice and rats [1][2][3]. The highest degree of activity was found in rats with autochthonous mam mary carcinomas.…”

Section: Gp 48 989 5-mcthyl-3-(2-methylallyl)-2-[(3-mcthyl-4-oxo-2-thmentioning

confidence: 99%

Regression of “Hormone-Independent” DMBA-induced Mammary Carcinomas in Response to GP 48989 and its Effect on Hormone Receptors

Schmidt-Ruppin¹,

Joss²,

Schieweck³

1976

Oncology

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Effects of GP 48 989 Alone and in Combination with Hormones and Chemotherapeutic Agents on DMBA-Induced Mammary Carcinomata II

Schmidt-Ruppin

Schieweck

1976

Chemotherapy

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Carcinostatic activity of a thiazolidinonylidene-hydrazonothiazolidinone derivative against DMBA-induced mammary carcinomata in female Sprague-Dawley rats

Cited by 5 publications

References 1 publication

Thiazolidine Diones, Specific Ligands of the Nuclear Receptor Retinoid Z Receptor/Retinoid Acid Receptor-related Orphan Receptor α with Potent Antiarthritic Activity

Thiazolidine Diones, Specific Ligands of the Nuclear Receptor Retinoid Z Receptor/Retinoid Acid Receptor-related Orphan Receptor α with Potent Antiarthritic Activity

Regression of “Hormone-Independent” DMBA-induced Mammary Carcinomas in Response to GP 48989 and its Effect on Hormone Receptors

Effects of GP 48 989 Alone and in Combination with Hormones and Chemotherapeutic Agents on DMBA-Induced Mammary Carcinomata II

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