Trabectedin D3 (Ecteinascidin 743 D3) 是 Trabectedin 的氘代物。Trabectedin (Ecteinascidin 743; ET-743) 是一种四氢异喹啉生物碱，具有有效的抗肿瘤活性。Trabectedin 与 DNA 的小沟结合，阻断应激诱导的蛋白质的转录，诱导 DNA 骨架裂解和癌细胞凋亡 (apoptosis)，并增加 MCF-7 和 MDA-MB-453 细胞中 ROS 的生成。Trabectedin 可用于软组织肉瘤和卵巢癌的研究。
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetradroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer treatment[1][2][3].
[1]. Takahashi N, et al. Sequence-dependent synergistic cytotoxicity of ecteinascidin-743 and NSC 125973 in human breast cancer cell linesin vitro and in vivo. Cancer Res. 2002 Dec 1;62(23):6909-15.
[2]. Atmaca H, et al. A diverse induction of apoptosis by trabectedin in MCF-7 (HER2-/ER+) and MDA-MB-453 (HER2+/ER-) breast cancer cells. Toxicol Lett. 2013 Jun 20;221(2):128-136.
[3]. Germano G, et al. Antitumor and anti-inflammatory effects of trabectedin on human myxoid liposarcoma cells. Cancer Res. 2010 Mar 15;70(6):2235-44.
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