Högger P, Erpenstein U, Rohdewald P, Sorg C
Institute of Pharmaceutical Chemistry, Münster, Germany.
Pharm Res. 1998 Feb;15(2):296-302. doi: 10.1023/a:1011931021743.
Upon glucocorticoid stimulation, human mononuclear leucocytes express an antigen, RM3/1, which characterizes a subpopulation of human monocytes and macrophages evolving in late phase of inflammation. We investigated biochemical properties of the RM3/1 antigen and correlations between antigen expression and glucocorticoid potency.
Biochemical properties were analyzed after solubilization by immunoaffinity methods and SDS-PAGE.
Induction of the RM3/1 antigen is a glucocorticoid receptor mediated process, in contrast, inflammatory mediators such as LPS or TPA were not able to upregulate RM3/1 expression. After SDS-PAGE, the antigen appeared as a 130 kDa (nonreduced)/150 kDa (reduced) glycoprotein with a 25 kDa N-linked glycoportion. The interdependence between antigen density and glucocorticoid efficacy was assessed by calculation of relative antigen expression induced by dexamethasone, fluticasone propionate, budesonide, triamcinolone acetonide, flunisolide, beclomethasone, prednisolone and triamcinolone. Relative antigen expression was significantly correlated with the relative receptor affinity of the glucocorticoid.
We described biochemical properties of the glucocorticoid-induced protein RM3/1. Though the precise role of the RM3/1 antigen in the antiinflammatory process is not fully understood yet, an useful application of the induced expression could already be demonstrated for pre-clinical screening of glucocorticoid potency.
在糖皮质激素刺激下，人单核白细胞表达一种抗原RM3/1，该抗原可表征在炎症后期演变的人单核细胞和巨噬细胞亚群。我们研究了RM3/1抗原的生化特性以及抗原表达与糖皮质激素效力之间的相关性。
通过免疫亲和法和SDS-PAGE溶解后分析生化特性。
RM3/1抗原的诱导是一个糖皮质激素受体介导的过程，相比之下，诸如LPS或TPA等炎症介质无法上调RM3/1的表达。经SDS-PAGE后，该抗原呈现为一种130 kDa（非还原型）/150 kDa（还原型）的糖蛋白，带有一个25 kDa的N-连接糖部分。通过计算地塞米松、丙酸氟替卡松、布地奈德、曲安奈德、氟尼缩松、倍氯米松、泼尼松龙和曲安西龙诱导的相对抗原表达，评估了抗原密度与糖皮质激素效力之间的相互依赖性。相对抗原表达与糖皮质激素的相对受体亲和力显著相关。
我们描述了糖皮质激素诱导蛋白RM3/1的生化特性。尽管RM3/1抗原在抗炎过程中的确切作用尚未完全了解，但诱导表达在糖皮质激素效力的临床前筛选中已显示出有用的应用价值。
