University Children's Hospital, Zurich, Switzerland.
Horm Res Paediatr. 2010;73(3):198-204. doi: 10.1159/000284362. Epub 2010 Mar 3.
P450c17 has two distinct activities: 17alpha-hydroxylase activity and 17,20-lyase activity. Combined 17alpha-hydroxylase/17,20-lyase deficiency leads to a severe defect in the production of cortisol and sex steroids. In affected males this results in impaired masculinization with ambiguous or female external genitalia. Female patients have normal genitalia but show a lack of pubertal development in adolescence. An increased production of mineralocorticoids often leads to hypertension and hypokalemia in both sexes.
To better understand the mechanisms of P450c17 deficiency, we studied 2 patients (both 46,XY) with combined 17alpha-hydroxylase/17,20-lyase deficiency of different severity: one with complete lack of masculinization and one with ambiguous genitalia.
Four mutations were identified by sequencing of the CYP17A1 gene: I332T and A355T in the less severely affected patient; G111S and R440H in the patient with complete lack of masculinization. The three novel mutations were expressed in COS1 cells and all mutant proteins except I332T showed a complete loss of both enzymatic activities. I332T retained some residual 17alpha-hydroxylase as well as 17,20-lyase activity.
We identified 2 patients with the phenotypical spectrum of P450c17 deficiency. Three novel mutations in the CYP17A1 gene were identified and their functional characterization provided a good phenotype-genotype correlation. The location of the mutated residues in the three-dimensional model of P450c17 gave some additional insights into its structure-function relationship.
P450c17 具有两种截然不同的活性:17α-羟化酶活性和 17,20-裂合酶活性。17α-羟化酶/17,20-裂合酶联合缺乏导致皮质醇和性激素产生的严重缺陷。受影响的男性表现出雄性化障碍,外生殖器模糊或女性化。女性患者外生殖器正常,但青春期青春期发育不良。糖皮质激素的产生增加通常会导致两性高血压和低钾血症。
为了更好地理解 P450c17 缺乏的机制,我们研究了 2 名(均为 46,XY)具有不同严重程度的 17α-羟化酶/17,20-裂合酶联合缺乏的患者:一名完全没有雄性化,另一名生殖器模糊。
通过 CYP17A1 基因测序鉴定了 4 种突变:在病情较轻的患者中,I332T 和 A355T;在完全没有雄性化的患者中,G111S 和 R440H。三种新的突变在 COS1 细胞中表达,除 I332T 外,所有突变蛋白均完全丧失了两种酶活性。I332T 保留了一些残余的 17α-羟化酶和 17,20-裂合酶活性。
我们鉴定了 2 名具有 P450c17 缺乏表型谱的患者。在 CYP17A1 基因中发现了 3 种新的突变,其功能特征提供了良好的表型-基因型相关性。突变残基在 P450c17 三维模型中的位置为其结构-功能关系提供了一些额外的见解。