The bromodomain and extraterminal (BET) family of proteins are epigenetic readers of acetylated histones and are critical activators of oncogenic networks across many cancers. 对急性乳腺癌的致病网络来说，BET蛋白家族是一些非常关键的表观遗传阅读者。靶向BET蛋白已经成为治疗终末期去势抵抗前列腺癌的兴趣点，近年来发现了许多结构各异的BET抑制剂并加以测试。预临床研究表明，BET抑制剂对前列腺癌具有显著的抗增殖活性。然而，它们作为单药疗法的临床成功受到了治疗相关毒副作用、自身和后得到的药物耐受性以及缺乏预测性获益的生物标志物的限制。本文概述了BET抑制剂设计、预临床研究以及前列腺癌临床试验结论的进展。我们推测将BET抑制剂与其他药物组合应用以提高BET抑制在治疗前列腺癌中的治疗指数。BET抑制剂治疗前列腺癌的治疗潜力已在预临床研究中得到证明，但需要进一步研究以确定可以预测对BET抑制剂敏感性的生物标志物，并开发新型高度选择性抑制剂以降低毒副作用。最后，BET抑制剂与其他药物组合起来可能具有最大的临床潜力。

The bromodomain and extraterminal (BET) family of proteins are epigenetic readers of acetylated histones and are critical activators of oncogenic networks across many cancers. Therapeutic targeting of BET proteins has been an attractive area of clinical development for metastatic castration-resistant prostate cancer. In recent years, many structurally diverse BET inhibitors have been discovered and tested. Preclinical studies have demonstrated significant antiproliferative activity of BET inhibitors against prostate cancer. However, their clinical success as monotherapies has been limited by treatment-associated toxicities, primary and acquired drug resistance, and a lack of predictive biomarkers of benefit.This review provides an overview of advancements in BET inhibitor design, preclinical research, and conclusions from clinical trials in prostate cancer. We speculate on incorporating BET inhibitors into combination regimens with other agents to improve the therapeutic index of BET inhibition in treating prostate cancer.The therapeutic potential of BET inhibitors for prostate cancer has been demonstrated in preclinical studies. However, further research is needed to identify biomarkers that can predict sensitivity to BET inhibitors and to develop novel, highly selective inhibitors to reduce toxicities. Finally, BET inhibitors are likely to hold the most clinical potential in combination with other agents.