Evangelos Briasoulis - Cyanobacterial Cyclopeptides as Lead Compounds to Novel Targeted Cancer Drug

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      Cyanobacterial cyclopeptides, including microcystins and   nodularins, are considered a health hazard to humans due to the   possible toxic effects of high consumption. From a   pharmacological standpoint, microcystins are stable hydrophilic   cyclic heptapeptides with a potential to cause cellular damage   following uptake via organic anion-transporting polypeptides   (OATP). Their intracellular biological effects involve inhibition   of catalytic subunits of protein phosphatase 1 (PP1) and PP2,   glutathione depletion and generation of reactive oxygen species   (ROS). Interestingly, certain OATPs are prominently expressed in   cancers as compared to normal tissues, qualifying MC as potential   candidates for cancer drug development. In the era of targeted   cancer therapy, cyanotoxins comprise a rich source of natural   cytotoxic compounds with a potential to target cancers expressing   specific uptake transporters. Moreover, their structure offers   opportunities for combinatorial engineering to enhance the   therapeutic index and resolve organ-specific toxicity issues. In   this article, we revisit cyanobacterial cyclopeptides as   potential novel targets for anticancer drugs by summarizing   existing biomedical evidence, presenting structure-activity data   and discussing developmental perspectives.

      Address (URL): http://www.mdpi.com/1660-3397/8/3/629/