首页> 美国卫生研究院文献>BMC Pharmacology Toxicology >A novel 11β-hydroxysteroid dehydrogenase type1 inhibitor CNX-010-49 improves hyperglycemia lipid profile and reduces body weight in diet induced obese C57B6/J mice with a potential to provide cardio protective benefits
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A novel 11β-hydroxysteroid dehydrogenase type1 inhibitor CNX-010-49 improves hyperglycemia lipid profile and reduces body weight in diet induced obese C57B6/J mice with a potential to provide cardio protective benefits

机译:新型11β-羟类固醇脱氢酶type1抑制剂CNX-010-49可改善饮食诱发的肥胖C57B6 / J小鼠的高血糖血脂状况并减轻其体重具有提供心脏保护作用的潜力

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摘要

Background11ß–hydroxysteroid dehydrogenase type1 (11β-HSD1) converts inactive glucocorticoids to active glucocorticoids which, in excess, leads to development of the various risk factors of the metabolic syndrome. Recent studies clearly suggest that both increased expression and activity of 11β-HSD1 in metabolically active tissues such as liver, muscle and adipose are implicated in tissue specific dysregulation which collectively contribute to the whole body pathology seen in metabolic syndrome. In the present study we have evaluated CNX-010-49, a highly potent, selective and ‘pan tissue’ acting 11β-HSD1 inhibitor, for its potential to modulate multiple risk factors of the metabolic syndrome.
机译:背景11β-羟基类固醇脱氢酶1(11β-HSD1)将非活性糖皮质激素转化为活性糖皮质激素,过多地导致了代谢综合征的各种危险因素的发展。最近的研究清楚地表明,11β-HSD1在肝脏,肌肉和脂肪等代谢活跃组织中的表达和活性均与组织特异性失调有关,这些失调共同导致了代谢综合征中所见的全身病理。在本研究中,我们评估了CNX-010-49(一种高效,选择性和“泛组织”作用的11β-HSD1抑制剂)具有调节多种代谢综合征危险因素的潜力。

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