Cyanobacterial cyclopeptides as lead compounds to novel targeted cancer drugs

Mar Drugs. 2010 Mar 15;8(3):629-57. doi: 10.3390/md8030629.


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: OATP; cancer; cyanobacteria; cyanotoxins; membrane transporters; microcystin; targeted-therapy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Bacterial Toxins / chemistry
  • Bacterial Toxins / pharmacology
  • Cell Proliferation / drug effects
  • Cyanobacteria / chemistry*
  • Cyanobacteria Toxins
  • Drug Delivery Systems
  • Drug Discovery
  • Marine Toxins / chemistry
  • Marine Toxins / pharmacology
  • Microcystins / chemistry
  • Microcystins / pharmacology
  • Neoplasms / drug therapy
  • Peptides / chemistry*
  • Peptides / pharmacology


  • Antineoplastic Agents
  • Bacterial Toxins
  • Cyanobacteria Toxins
  • Marine Toxins
  • Microcystins
  • Peptides
  • microcystin