聚腺苷二磷酸核糖聚合酶抑制剂在癌症治疗中的应用。
PARP Inhibitors for Cancer Therapy.
机构信息
University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
出版信息
Cell. 2017 Apr 6;169(2):183. doi: 10.1016/j.cell.2017.03.034.
PMID:28388401
Abstract
Rucaparib is an inhibitor of nuclear poly (ADP-ribose) polymerases (inhibition of PARP-1 > PARP-2 > PARP-3), following a similar drug, Olaparib. It disrupts DNA repair and replication pathways (and possibly transcription), leading to selective killing of cancer cells with BRCA1/2 mutations. Rucaparib is approved for recurrent ovarian cancers with germline or somatic mutations in BRCA1/2.
摘要
鲁卡帕尼是一种核多聚（ADP-核糖）聚合酶抑制剂（对 PARP-1 > PARP-2 > PARP-3 的抑制作用），类似于奥拉帕利。它破坏 DNA 修复和复制途径（可能还有转录），导致具有 BRCA1/2 突变的癌细胞选择性死亡。鲁卡帕尼获批用于治疗存在 BRCA1/2 种系或体细胞突变的复发性卵巢癌。
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