[關鍵詞]
[摘要]
腫瘤細胞能夠激活自身DNA的損傷修復機制進行修復,從而導致其對抗腫瘤藥物和放療產生耐藥性,而聚腺苷酸二磷酸核糖轉移酶(poly ADP-ribose polymerase,PARP)是一種DNA修復酶,在DNA修復通路中起關鍵作用。veliparib是一種新型高選擇抑制PARP的苯并咪唑類化合物,體內外實驗表明本品具有顯著的抑制PARP活性的作用。在治療轉移性乳腺癌、結腸癌、轉移性黑色素瘤和腦腫瘤方面已取得顯著的效果,其與替莫唑胺聯用治療乳腺癌的研究即將進入III期臨床。
[Key word]
[Abstract]
Tumor cells are able to activate their own DNA damage repair so as to repaire themselves, thus causing drug resistance against antitumor drugs and radiotherapy. While polyadenylation diphosphate ribose transferase (poly ADP-ribose polymerase, PARP) is a DNA repair enzyme which plays a key role in DNA repair pathways. Veliparib is a novel oral benzimidazole derivative that is a highly potent and selective PARP. The in vivo and in vitro experiments show that veliparib has a significant inhibition on PARP activity. In the treatment of metastatic breast cancer, colon cancer, metastatic melanoma, and brain tumor, the compound has made a significant effect, and its combination with temozolomide is going to enter phase III in clinic for the treatment of breast cancer.
[中圖分類號]
[基金項目]