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糖皮质激素抵抗的机制已引起广泛关注。糖皮质激素受体(GR)异常是糖皮质激素抵抗的机制之一,而GR基因突变可引起糖皮质激素的结构和功能异常。近年来大量体外GR基因突变研究证明,诱变位于GR“结合口袋”附近的氨基酸,大部分情况会引起GR功能下降,但是突变个别氨基酸可引起GR和糖皮质激素亲和力升高。是否可用改造过的GR进行基因治疗,以减少糖皮质激素抵抗带来的不良反应,是一个值得考虑的问题。现就GR的氨基酸结构和功能的关系作一综述。
The mechanism of glucocorticoid resistance has drawn wide attention. Glucocorticoid receptor (GR) abnormalities are one of the mechanisms of glucocorticoid resistance, and mutations in the GR gene can cause glucocorticoid structural and functional abnormalities. In recent years, a large number of in vitro GR gene mutation studies have shown that mutagenesis located in the GR “binding pocket” amino acids, in most cases will cause decreased GR function, but mutations in individual amino acids can cause GR and glucocorticoid affinity increased. The availability of genetically modified GR for gene therapy to reduce the adverse effects of glucocorticoid resistance is a question worth considering. Now on the GR amino acid structure and function of a review.