期刊
CANCER BIOLOGY & THERAPY
卷 3, 期 6, 页码 503-504出版社
TAYLOR & FRANCIS INC
DOI: 10.4161/cbt.3.6.961
关键词
HIF-1 alpha; hypoxia; HIF-1; angiogenesis; glycolysis; VEGF; cancer; VHL; PX-478; drug development
类别
Despite reservations regarding potential toxicities, small molecule-mediated blockade of the hypoxia-inducible factor-1 transcription factor has emerged as a viable anti-cancer strategy in vivo. Recent experiments by Welsh et al.(1) revealed unprecedented anti-tumor responses of various aggressive solid tumors to the HIF-1 -inhibitory small molecule drug PX-478. Compared with other anti-cancer drugs, PX-478 had markedly improved regression, growth delay and log(10) cell kill profiles, particularly against large tumors that are normally refractory to small molecule drug therapy. Importantly, pharmacokinetic and toxicity profiles were within acceptable limits, providing rationale for the clinical development of HIF-1 inhibitors in general. Though the mechanism of action for PX-478 is not completely understood, inhibition of glycolysis rather than angiogenesis appeared to be the primary mode of anti-cancer activity.
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