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Structures of androgen receptor bound with ligands: advancing understanding of biological functions and drug discovery

机译：雄激素受体与配体结合的结构：进一步了解生物学功能和药物发现

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Introduction: Androgen receptor (AR) is a ligand-dependent transcription factor and a member of the nuclear receptor superfamily. It plays a vital role in male sexual development and regulates gene expression in various tissues, including prostate. Androgens are compounds that exert their biological effects via interaction with AR. Binding of androgens to AR initiates conformational changes in AR that affect binding of co-regulator proteins and DNA. AR agonists and antagonists are widely used in a variety of clinical applications (i.e. hypogonadism and prostate cancer therapy).Areas covered: This review provides a close look at structures of AR-ligand complexes and mutations in the receptor that have been revealed, discusses current challenges in the field, and sheds light on future directions.Expert opinion: AR is one of the primary targets for the treatment of prostate cancer, as AR antagonists inhibit prostate cancer growth. However, these drugs are not effective for long-term treatment and lead to castration-resistant prostate cancer. The structures of AR-ligand complexes are an invaluable scientific asset that enhances our understanding of biological functions and mechanisms of androgenic and anti-androgenic chemicals as well as promotes the discovery of superior drug candidates.
机译：简介：雄激素受体（AR）是依赖配体的转录因子，是核受体超家族的成员。它在男性性发育中起着至关重要的作用，并调节包括前列腺在内的各种组织中的基因表达。雄激素是通过与AR相互作用发挥其生物学作用的化合物。雄激素与AR的结合引发AR中的构象变化，其影响共调节蛋白和DNA的结合。 AR激动剂和拮抗剂广泛用于各种临床应用中（即性腺功能低下和前列腺癌治疗）。涵盖领域：本综述仔细研究了AR-配体复合物的结构和受体中的突变，讨论了当前专家意见：由于AR拮抗剂抑制前列腺癌的生长，AR是治疗前列腺癌的主要靶标之一。但是，这些药物对长期治疗无效，并导致去势抵抗性前列腺癌。 AR-配体复合物的结构是一项宝贵的科学资产，可增进我们对雄激素和抗雄激素化学物质的生物学功能和机理的理解，并促进发现优秀的候选药物。

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