Graduate Program in Cell and Molecular Biology, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, Brazil.
Center for Biotechnology, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre 91501-970, Brazil.
Int J Mol Sci. 2021 Dec 28;23(1):296. doi: 10.3390/ijms23010296.
Deficiency of 21-hydroxylase enzyme (CYP21A2) represents 90% of cases in congenital adrenal hyperplasia (CAH), an autosomal recessive disease caused by defects in cortisol biosynthesis. Computational prediction and functional studies are often the only way to classify variants to understand the links to disease-causing effects. Here we investigated the pathogenicity of uncharacterized variants in the CYP21A2 gene reported in Brazilian and Portuguese populations. Physicochemical alterations, residue conservation, and effect on protein structure were accessed by computational analysis. The enzymatic performance was obtained by functional assay with the wild-type and mutant CYP21A2 proteins expressed in HEK293 cells. Computational analysis showed that p.W202R, p.E352V, and p.R484L have severely impaired the protein structure, while p.P35L, p.L199P, and p.P433L have moderate effects. The p.W202R, p.E352V, p.P433L, and p.R484L variants showed residual 21OH activity consistent with the simple virilizing phenotype. The p.P35L and p.L199P variants showed partial 21OH efficiency associated with the non-classical phenotype. Additionally, p.W202R, p.E352V, and p.R484L also modified the protein expression level. We have determined how the selected CYP21A2 gene mutations affect the 21OH activity through structural and activity alteration contributing to the future diagnosis and management of CYP21A2 deficiency.
21-羟化酶缺乏症(CYP21A2)代表先天性肾上腺皮质增生症(CAH)的 90%病例,这是一种常染色体隐性疾病,由皮质醇生物合成缺陷引起。计算预测和功能研究通常是唯一的分类方法,用于了解与致病效应的联系。在这里,我们研究了在巴西和葡萄牙人群中报道的 CYP21A2 基因未表征变异的致病性。通过计算分析评估了物理化学改变、残基保守性和对蛋白质结构的影响。通过用野生型和突变 CYP21A2 蛋白在 HEK293 细胞中表达的功能测定获得了酶活性。计算分析表明,p.W202R、p.E352V 和 p.R484L 严重破坏了蛋白质结构,而 p.P35L、p.L199P 和 p.P433L 则具有中度影响。p.W202R、p.E352V、p.P433L 和 p.R484L 变体表现出与简单男性化表型一致的残余 21OH 活性。p.P35L 和 p.L199P 变体表现出与非典型表型相关的部分 21OH 效率。此外,p.W202R、p.E352V 和 p.R484L 还改变了蛋白质表达水平。我们已经确定了所选 CYP21A2 基因突变如何通过结构和活性改变影响 21OH 活性,从而为 CYP21A2 缺乏症的未来诊断和管理做出贡献。