Division of Endocrinology, Diabetes and Metabolism, University of Cincinnati, Cincinnati, OH 45267-0567, USA.
Trends Endocrinol Metab. 2010 Nov;21(11):691-8. doi: 10.1016/j.tem.2010.08.004. Epub 2010 Sep 16.
Breast and prostate cancers are hormone-sensitive malignancies that afflict millions of women and men. Although prolactin (PRL) is known as a survival factor that supports tumor growth and confers chemoresistance in both cancers, its precise role in these tumors has not been studied extensively. Growth hormone and placental lactogen also bind PRL receptor (PRLR) and mimic some of the actions of PRL. Blockade of the PRLR represents a novel treatment for patients with advanced breast or prostate cancer with limited therapeutic options. This review discusses different approaches for generating PRLR antagonists. Emphasis is placed on technological advances which enable high-throughput screening for small molecule inhibitors of PRLR signaling that could serve as oral medications.
乳腺癌和前列腺癌是两种激素敏感性恶性肿瘤,困扰着数以百万计的女性和男性。虽然催乳素(PRL)被认为是一种生存因子,可支持两种癌症中的肿瘤生长并赋予其化疗耐药性,但它在这些肿瘤中的确切作用尚未得到广泛研究。生长激素和胎盘催乳素也与催乳素受体(PRLR)结合,并模拟 PRL 的一些作用。PRLR 阻断代表了一种治疗晚期乳腺癌或前列腺癌的新方法,这些癌症的治疗选择有限。本文综述了生成 PRLR 拮抗剂的不同方法。重点介绍了能够进行 PRLR 信号小分子抑制剂高通量筛选的技术进步,这些抑制剂可能成为口服药物。