Mitochondrially targeted anti-cancer agents

Cancer is an ever-increasing problem that is yet to be harnessed Frequent mutations make this pathology very variable and consequently a considerable challenge Intriguingly mitochondria have recently emerged as novel targets for cancer therapy A group of agents with anti-cancer activity that induce apoptosis by way of mitochondrial destabilisation termed mitocans have been a recent focus of research Of these compounds many are hydrophobic agents that associate with various sub cellular organelles Clearly modification of such structures with mitochondria targeting moieties for example tagging them with lipophilic cations would be expected to enhance their activity This may be accomplished by the addition of triphenylphosphonium groups that direct such compounds to mitochondria enhancing their activity In this paper we will review agents that possess anti-cancer activity by way of destabilising mitochondria and their possible targets We propose that mitochondrial targeting in particular where the agent associates directly with the target results in more specific and efficient anti-cancer drugs of potential high clinical relevance (C) 2010 Elsevier BV and Mitochondria Research Society All rights reserved