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雄激素控制着广泛的生理学功能。雄激素受体作为调节雄激素多种生物学作用的甾体类受体 ,是一种配基诱导的转录因子。雄激素信号系统的异常导致了从性别确定和性征发育到精神和情感失常的许多紊乱。雄激素替代治疗能改善许多临床症状 ,包括性腺机能低下与骨质疏松 ,但由于疗效不高和缺少方便给药的安全制剂而受到限制。最近甾体类受体和选择性受体调节子的基因调控技术 ,为选择性雄激素受体调节子能否解答现行雄激素治疗中存在的问题 ,提供了验证的机会。配基化的雄激素受体转录引发复合物的组成决定了基因调控的特异性 ,设计用于引发组织和启动子特异基因转录的合成配基提供了开发更有效的雄激素治疗的希望。建立能预测合成配基活性的测试方法是选择性雄激素受体调节子开发的关键。化合物筛选的高效率和基因指纹技术的进步 ,如微阵列技术和蛋白质组学 ,将加速有效的选择性受体调节子鉴定。
Androgens control a wide range of physiological functions. Androgen receptor As a steroid receptor that regulates the multiple biological roles of androgens, it is a ligand-induced transcription factor. Abnormalities in the androgen signaling system have led to many disorders ranging from gender determination and sexual development to mental and emotional disorders. Androgen replacement therapy can improve many clinical symptoms, including hypogonadism and osteoporosis, but is limited by poor efficacy and lack of safe dosage for ease of administration. The recent gene regulation of steroid receptors and selective receptor regulators provides an opportunity for validation as to whether selective androgen receptor regulators can answer the questions of current androgen therapy. The composition of the ligandized androgen receptor transcription-initiating complex determines the specificity of gene regulation and the design of synthetic ligands for initiation of transcription of tissue and promoter-specific genes provides the hope of developing more effective androgen therapy. Establishing a test that predicts the activity of synthetic ligands is key to the development of selective androgen receptor modulators. Advances in compound screening and advances in genetic fingerprinting techniques, such as microarray technology and proteomics, will speed up the identification of effective selective receptor modulators.