Ponec M
Br J Dermatol. 1982 Nov;107 Suppl 23:24-9. doi: 10.1111/j.1365-2133.1982.tb01027.x.
Cytosol fractions of both cultured human skin fibroblasts and epidermal keratinocytes contain macromolecules that bind glucocorticoids with high affinity. Using the cytosol of cultured keratinocytes good correlation has been found between the displacement of radiolabelled glucocorticoids (3H-hydrocortisone, 3H-dexamethasone and 3H-triamcinolone acetonide) by a variety of glucocorticoids and the clinical efficacy. The structure-binding relationship studies revealed the relative contribution of various substituents on the steroid molecule for the binding affinity of the steroids. The introduction of a double bond at C1-C2, the presence of 9 alpha-fluoro atom or 11 beta-hydroxy group and the esterification of the 17 alpha-hydroxy group caused an increase, whereas esterification of the hydroxy group on C21 leads to marked decrease of the affinity of the steroid.
培养的人皮肤成纤维细胞和表皮角质形成细胞的胞质溶胶组分都含有能与糖皮质激素高亲和力结合的大分子。利用培养的角质形成细胞的胞质溶胶，已发现多种糖皮质激素对放射性标记的糖皮质激素（3H-氢化可的松、3H-地塞米松和3H-曲安奈德）的置换与临床疗效之间有良好的相关性。结构-结合关系研究揭示了甾体分子上各种取代基对甾体结合亲和力的相对贡献。在C1-C2处引入双键、存在9α-氟原子或11β-羟基以及17α-羟基的酯化会导致亲和力增加，而C21上羟基的酯化会导致甾体亲和力显著降低。
