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Journal Club
Small Molecule-Mediated Anti-Cancer Therapy via Hypoxia Inducible Factor-1 Blockade
Gordon R. Macpherson and William D. Figg
volume 3 | issue 6
june 2004Pages: 503-504
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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 log10 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.
We now provide open access to journal articles published online for one year or more. This article may be downloaded at the following link:
Download PDFIf the document does not open, please right-click on the link (control-click on a Macintosh) and select the option to save the file to disk.