GPR30是人类原位癌和精原细胞瘤的潜在治疗靶点

P. Chieffi
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引用次数: 3

摘要

G蛋白偶联雌激素受体(GPR30)被认为在非核雌激素信号传导中发挥作用,并在多种激素依赖性癌症实体中过表达。雌激素与睾丸生殖细胞肿瘤的发生有密切关系。在最近发表在《细胞生理学杂志》上的一篇论文中,我们发现雌激素受体β (ERβ)的下调与人类睾丸原位癌(CIS)和精原细胞瘤中GPR30的过表达相关。此外,我们证明17b-雌二醇通过GPR30诱导ERK1/2活化。结果表明,暴露于雌激素或雌激素模拟物,以某种尚未明确的方式,减少了erb介导的CIS和人睾丸精原细胞瘤的生长抑制,这表明GPR30可能是设计特异性抑制剂的潜在治疗靶点。
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GPR30 is a potential therapeutic target in human carcinoma in situ and seminomas
The G protein-coupled estrogen receptor (GPR30) is suggested to exert a role in non-nuclear estrogen signalling and is over-expressed in a variety of hormone dependent cancer entities. It is well established that oestrogens are involved in testicular germ cell tumours. In a recent paper published in Journal of Cellular Physiology, we show that down regulation of estrogen receptor β (ERβ) associates with GPR30 over-expression both in human testicular carcinoma in situ (CIS) and seminomas. In addition, we demonstrate that 17b-oestradiol induces the ERK1/2 activation through GPR30. The results suggested that exposure to oestrogens or oestrogen-mimics, in some as of yet undefined manner, diminishes the ERb-mediated growth restraint in CIS and in human testicular seminoma, indicating that GPR30 could be a potential therapeutic target to design specific inhibitors.
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