期刊
PURE AND APPLIED CHEMISTRY
卷 84, 期 6, 页码 1369-1378出版社
WALTER DE GRUYTER GMBH
DOI: 10.1351/PAC-CON-11-10-31
关键词
apoptosis; anticancer activity; antitumor activity; bioactive molecules; chaetocin; histone methyltransferase
资金
- Grants-in-Aid for Scientific Research [22590034] Funding Source: KAKEN
Chaetocin, a natural product isolated from fungi of Chaetomium species, is a member of the epipolythiodiketopiperazines (ETPs), which have various biological activities, including cytostatic and anticancer activities. Recently, the inhibitory activity toward histone methyltransferases (HMTs) was discovered for chaetocin. We previously reported the first total synthesis of chaetocin and various derivatives. During studies on the structure-activity relationship for HMT inhibition, we found that the enantiomer of chaetocin (ent-chaetocin) is a more potent apoptosis inducer than natural chaetocin in human leukemia HL-60 cells. Mechanistic studies showed that ent-chaetocin induces apoptosis through the caspase-8/caspase-3 pathway.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据