甾体激素拮抗剂的开发现状及作用机制

来源 :上海医药情报研究 | 被引量 : 0次 | 上传用户:wanglinux_0208
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甾体激素拮抗剂包括抑制产生甾体激素的药物和拮抗甾体激素受体的药物这两类。两类药物除用于治疗与对应激素过剩有关的疾病和激素依赖性肿瘤之外,还是研究激素受体和解析激素作用机制的工具之一。受体拮抗剂因其特异性,临床应用潜力甚大。甾体激素受体大致可分为比较大的皮质激素、孕激素和雄激素受体与稍小的雌激素受体两组。由于同组受体间的相同性非常高,故它们的拮抗剂多同时对数个受体显现激动活性或拮抗活性。为此,基础研究现正在致力于确认各种甾体激素的特异性受体,期望通过基因克隆搞清其分子中的DNA结合部位和配体结合部位。另外,从解析甾体激素受体的三维 Steroid hormone antagonists include both drugs that inhibit the production of steroid hormones and drugs that antagonize steroid hormone receptors. In addition to being used to treat diseases and hormone-dependent cancers that are associated with excess of the hormone, both drugs are also one of the tools for studying the mechanisms of action of hormone receptors and resolving hormones. Receptor antagonists have great potential for clinical application due to their specificity. Steroid hormone receptors can be broadly divided into larger corticosteroids, progesterone and androgen receptor and slightly smaller estrogen receptor two groups. Because of the very high identity between receptors in the same group, many of their antagonists show agonistic activity or antagonistic activity to several receptors at the same time. For this reason, basic research is currently focused on identifying specific receptors for various steroid hormones, and it is expected that DNA binding sites and ligand binding sites in the molecule will be identified by gene cloning. In addition, three-dimensional analysis of steroid hormone receptors
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