Department of Pathology, Virginia Commonwealth University, Richmond, VA 23298, USA.
Wright Center for Clinical and Translational Research, Virginia Commonwealth University, Richmond, VA 23298, USA.
Endocrinology. 2024 Apr 29;165(6). doi: 10.1210/endocr/bqae039.
Prolactin and its receptor (PRLr) in humans are significantly involved in breast cancer pathogenesis. The intermediate form of human PRLr (hPRLrI) is produced by alternative splicing and has a novel 13 amino acid tail ("I-tail") gain. hPRLrI induces significant proliferation and anchorage-independent growth of normal mammary epithelia in vitro when coexpressed with the long form hPRLr (hPRLrL). hPRLrL and hPRLrI coexpression is necessary to induce the transformation of mammary epithelia in vivo. The I-tail is associated with the ubiquitin-like protein neural precursor cell expressed developmentally downregulated protein 8. Treatment with the neural precursor cell expressed developmentally downregulated protein 8-activating enzyme inhibitor pevonedistat resulted in increased hPRLrL and the death of breast cancer cells. The goal of this study was to determine the function of the hPRLrI I-tail in hPRLrL/hPRLrI-mediated mammary transformation. hPRLrL/hPRLrI and hPRLrL/hPRLrIΔ13 (I-tail removal mutant) were delivered to MCF10AT cells. Cell proliferation was decreased when hPRLrI I-tail was removed. I-tail deletion decreased anchorage-independent growth and attenuated cell migration. The I-tail was involved in Ras/MAPK signaling but not PI3K/Akt signaling pathway as shown by western blot. I-tail removal resulted in decreased hPRLrI stability. RNA-sequencing data revealed that I-tail removal resulted in differential gene expression induced by prolactin. Ingenuity Pathway Analysis revealed that the activity of ERK was attenuated. Treatment of breast cancer cells with ERK1/2 inhibitor ulixertinib resulted in decreased colony-forming ability and less proliferation. These studies suggest that the hPRLrI I-tail contributed to breast oncogenesis and may be a promising target for the development of new breast cancer therapies.
人类的催乳素及其受体(PRLr)在乳腺癌发病机制中起着重要作用。人类 PRLr 的中间形式(hPRLrI)通过选择性剪接产生,具有新的 13 个氨基酸尾巴(“I 尾巴”)获得。当与长形式 hPRLr(hPRLrL)共表达时,hPRLrI 可诱导体外正常乳腺上皮细胞的显著增殖和无锚定生长。hPRLrL 和 hPRLrI 的共表达是诱导体内乳腺上皮细胞转化所必需的。I 尾巴与泛素样蛋白神经前体细胞表达的发育下调蛋白 8 相关。用神经前体细胞表达的发育下调蛋白 8 激活酶抑制剂 pevonedistat 处理可导致 hPRLrL 增加和乳腺癌细胞死亡。本研究的目的是确定 hPRLrI I 尾巴在 hPRLrL/hPRLrI 介导的乳腺转化中的功能。将 hPRLrL/hPRLrI 和 hPRLrL/hPRLrIΔ13(I 尾巴缺失突变体)递送至 MCF10AT 细胞。当去除 hPRLrI I 尾巴时,细胞增殖减少。I 尾巴缺失减少了无锚定生长并减弱了细胞迁移。Western blot 显示,I 尾巴缺失减少了 Ras/MAPK 信号通路但不影响 PI3K/Akt 信号通路。I 尾巴缺失导致 hPRLrI 稳定性降低。RNA-seq 数据显示,I 尾巴缺失导致催乳素诱导的基因表达差异。Ingenuity Pathway Analysis 揭示 ERK 的活性减弱。用 ERK1/2 抑制剂 ulixertinib 处理乳腺癌细胞可导致集落形成能力降低和增殖减少。这些研究表明,hPRLrI I 尾巴促进了乳腺癌的发生,可能是开发新的乳腺癌治疗方法的有前途的靶点。