Mar. Drugs 2010, 8(3), 629-657; doi:10.3390/md8030629
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Cyanobacterial Cyclopeptides as Lead Compounds to Novel Targeted Cancer Drugs

1 Human Cancer Biobank Center, University of Ioannina, Greece 2 Department of Materials Science and Engineering, University of Ioannina, Greece 3 Department of Biological Applications and Technologies, University of Ioannina, Greece 4 Department of Chemistry, University of Ioannina, Greece 5 School of Medicine, University of Ioannina, Greece
* Author to whom correspondence should be addressed.
Received: 4 January 2010; in revised form: 10 February 2010 / Accepted: 26 February 2010 / Published: 15 March 2010
(This article belongs to the Special Issue Algal Toxins)
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Abstract: 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.
Keywords: microcystin; cyanobacteria; cyanotoxins; cancer; targeted-therapy; OATP; membrane transporters

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MDPI and ACS Style

Sainis, I.; Fokas, D.; Vareli, K.; Tzakos, A.G.; Kounnis, V.; Briasoulis, E. Cyanobacterial Cyclopeptides as Lead Compounds to Novel Targeted Cancer Drugs. Mar. Drugs 2010, 8, 629-657.

AMA Style

Sainis I, Fokas D, Vareli K, Tzakos AG, Kounnis V, Briasoulis E. Cyanobacterial Cyclopeptides as Lead Compounds to Novel Targeted Cancer Drugs. Marine Drugs. 2010; 8(3):629-657.

Chicago/Turabian Style

Sainis, Ioannis; Fokas, Demosthenes; Vareli, Katerina; Tzakos, Andreas G.; Kounnis, Valentinos; Briasoulis, Evangelos. 2010. "Cyanobacterial Cyclopeptides as Lead Compounds to Novel Targeted Cancer Drugs." Mar. Drugs 8, no. 3: 629-657.

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