谷氨酸羧肽酶Ⅱ
癌症研究
靶向治疗
前列腺癌
前列腺
内化
PI3K/AKT/mTOR通路
雄激素剥夺疗法
医学
化学
内科学
信号转导
受体
生物化学
癌症
作者
Justine Maes,Simon Gesquière,Anton De Spiegeleer,Alex Maes,Christophe Van de Wiele
摘要
Prostate-specific membrane antigen (PSMA), a transmembrane glycoprotein, was shown to be expressed 100–1000 fold higher in prostate adenocarcinoma as compared to normal prostate epithelium. Given the enzymatic function of PSMA with the presence of an internalization triggering motif, various Glu-urea-Lys-based inhibitors have been developed and, amongst others, radiolabeled with positron emitters for targeted positron emission tomography imaging such as 68Ga-PSMA-HBED-CC Glu-urea-Lys(Ahx) as well as with beta and alpha-emitting radioisotopes for targeted therapy, e.g., 177Lu-PSMA-617. In this paper, we review and discuss the potential implications for targeted imaging and therapy of altered PSMA-glycosylation, of PSMA-driven activation of the P13K/Akt/mTOR, of the evolution over time and the relationship with androgen signaling and changes in DNA methylation of PSMA, and of androgen deprivation therapy (ADT) in prostate carcinoma.
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