聚ADP核糖聚合酶
体内
化学
奥拉帕尼
PARP抑制剂
正电子发射断层摄影术
聚合酶
临床前影像学
软膜
生物物理学
癌症研究
分子生物学
生物化学
酶
核医学
生物
医学
生物技术
作者
Dong Zhou,Wenhua Chu,Jinbin Xu,Lynne A. Jones,Xin Peng,Shihong Li,Delphine L. Chen,Robert H. Mach
标识
DOI:10.1016/j.bmc.2014.01.019
摘要
Imaging of poly (ADP-ribose) polymerase-1 (PARP-1) expression in vivo is a potentially powerful tool for developing PARP-1 inhibitors for drug discovery and patient care. We have synthesized several derivatives of benzimidazole carboxamide as PARP-1 inhibitors, which can be 18F-labeled easily for positron emission tomographic (PET) imaging. Of the compounds synthesized, 12 had the highest inhibition potency for PARP-1 (IC50 = 6.3 nM). [18F]12 was synthesized under conventional conditions in high specific activity with 40–50% decay-corrected yield. MicroPET studies using [18F]12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [18F]12 in the tumor that was blocked by olaparib, suggesting that the uptake of [18F]12 in the tumor is specific to PARP-1 expression.
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