상세 보기
Effects of a Newly Developed Tricyclic PARP-1 Inhibitor, on Ischemic Stroke
- Yoo, A. Rum;
- Koh, Seong-Ho;
- Noh, Min Young;
- Cho, Goang Won;
- Park, Ji-Seon;
- ... Kim, Seung Hyun;
- 외 3명
Citations
WEB OF SCIENCE
1Citations
SCOPUS
1초록
Poly(ADP-ribose) polymerase (PARP)-1 plays an important role in the pathogenic mechanism of ischemic stroke. A number of studies have been undertaken to develop PARP-1 inhibitors for clinical use. We report on the newly developed PARP-1 inhibitors, among which 12a showed good activity (IC50) = 7.8 nM in an enzyme-based assay and = 0.73 mu M in a cell-based assay) and pharmacokinetic profiles. Treatment of the middle cerebral artery (MCA) occluded rats with 3 mg/kg 12a reduced infarct volume suggesting that, may be a good candidate for the treatment of ischemic stroke.
키워드
PARP; inhibitor; stroke; POLY(ADP-RIBOSE) SYNTHETASE ACTIVATION; CELL-DEATH; BIOLOGICAL EVALUATION; CEREBRAL-ISCHEMIA; DNA-DAMAGE; POLYMERASE-1; INFLAMMATION; DESIGN; POTENT; PEROXYNITRITE
- 제목
- Effects of a Newly Developed Tricyclic PARP-1 Inhibitor, on Ischemic Stroke
- 저자
- Yoo, A. Rum; Koh, Seong-Ho; Noh, Min Young; Cho, Goang Won; Park, Ji-Seon; Kim, Youngchul; Lee, Han-Chang; Kim, Myung-Hwa; Kim, Seung Hyun
- 발행일
- 2010-06
- 유형
- Article
- 권
- 71
- 호
- 4
- 페이지
- 253 ~ 260