Chieffi Paolo
Dipartimento di Psicologia, Università della Campania, Caserta, Italy.
Intractable Rare Dis Res. 2021 Nov;10(4):292-293. doi: 10.5582/irdr.2021.01103.
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 tumors. It is well known that estrogens and xenoestrogens are involved in testicular germ cell tumorigenesis. Different studies show that down regulation of estrogen receptor β (ERβ) associates with GPR30 over-expression both in human testicular carcinoma (CIS) and seminomas and that the mitogenic role exerted by 17β-oestradiol induces the activation of extracellular signal-regulated kinase 1/2 (ERK1/2) through GPR30. In conclusion, the exposure to oestrogens or oestrogen-mimics, in some as of yet undefined manner, diminishes the ERβ-mediated growth restraint in CIS and in human testicular seminoma, indicating that GPR30 could be considered a potential therapeutic target to design specific inhibitors.
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,且在多种激素依赖性肿瘤中过度表达。众所周知,雌激素和外源性雌激素参与睾丸生殖细胞肿瘤的发生。不同研究表明,在人类睾丸癌(原位癌)和精原细胞瘤中,雌激素受体β(ERβ)的下调与GPR30的过度表达相关,并且17β-雌二醇发挥的促有丝分裂作用通过GPR30诱导细胞外信号调节激酶1/2(ERK1/2)的激活。总之,以某种尚未明确的方式接触雌激素或雌激素模拟物会削弱ERβ介导的对原位癌和人类睾丸精原细胞瘤生长的抑制作用,这表明GPR30可被视为设计特异性抑制剂的潜在治疗靶点。