Centre for Cardiovascular Science, Queen's Medical Research Institute, University of Edinburgh, Edinburgh, United Kingdom.
Endocrinology. 2010 Jan;151(1):195-202. doi: 10.1210/en.2009-0663. Epub 2009 Nov 24.
Regeneration of active glucocorticoids within liver and adipose tissue by the enzyme 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) may be of pathophysiological importance in obesity and metabolic syndrome and is a therapeutic target in type 2 diabetes. Polymorphisms in HSD11B1, the gene encoding 11 beta-HSD1, have been associated with metabolic phenotype in humans, including type 2 diabetes and hypertension. Here, we have tested the functional consequences of two single nucleotide polymorphisms located in contexts that potentially affect tissue levels of 11 beta-HSD1. We report no effect of allelic variation at rs846910, a polymorphism within the 5'-flanking region of the gene on HSD11B1 promoter activity in vitro. However, compared with the common G allele, the A allele of rs13306421, a polymorphism located two nucleotides 5' to the translation initiation site, gave higher 11 beta-HSD1 expression and activity in vitro and was translated at higher levels in in vitro translation reactions, possibly associated with a lower frequency of "leaky scanning." These data suggest that this polymorphism may have direct functional consequences on levels of 11 beta-HSD1 enzyme activity in vivo. However, the rs13306421 A sequence variant originally reported in other ethnic groups may be of low prevalence because it was not detected in a population of 600 European Caucasian women.
肝脏和脂肪组织中酶 11β-羟甾类脱氢酶 1(11β-HSD1)将活性糖皮质激素再生,这在肥胖和代谢综合征的病理生理学中可能具有重要意义,也是 2 型糖尿病的治疗靶点。编码 11β-HSD1 的基因 HSD11B1 的多态性与人类的代谢表型有关,包括 2 型糖尿病和高血压。在这里,我们检测了位于可能影响 11β-HSD1 组织水平的环境中的两个单核苷酸多态性的功能后果。我们报告说,基因 5'侧翼区的 rs846910 多态性(位于翻译起始位点 5'的两个核苷酸处)的等位基因变异对 HSD11B1 启动子活性没有影响。然而,与常见的 G 等位基因相比,rs13306421 的 A 等位基因(位于翻译起始位点 5'的两个核苷酸处)在体外具有更高的 11β-HSD1 表达和活性,并且在体外翻译反应中翻译水平更高,可能与“漏扫描”的频率较低有关。这些数据表明,这种多态性可能对体内 11β-HSD1 酶活性水平具有直接的功能后果。然而,最初在其他种族群体中报道的 rs13306421A 序列变体可能由于在 600 名欧洲白种女性人群中未检测到而具有低流行率。