Date: 02 Jun 2013

Imiquimod: The biochemical mechanisms of immunomodulatory and anti-inflammatory activity

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Imidazoquinolines are a new group of compounds that recently have been introduced into clinical practice as antitumor and antiviral immunomodulators. Structurally, they are low molecular weight synthetic guanosine-like molecules. Although imiquimod, the most widely used imidazoquinoline, has been recommended for treatment of several forms of skin cancer and papillomas, its molecular mechanisms of action are not fully understood. In particular, imiquimod is known as a specific agonist of Toll-like receptor 7 (TLR7) and this capacity is widely used in a large number of experimental studies and clinical trials. Nevertheless, detailed analysis of the published data suggests that the biological activity of imiquimod can not be explained only by its interaction with TLR7. Certain evidence exists that imiquimod directly interacts with adenosine receptors and other molecules that regulate synthesis of cyclic adenosine monophosphate. A detailed understanding of the biochemical basis of immunomodulating and antitumor effects of imiquimod will increase its clinical effectiveness and accelerate the development of new drugs with similar but improved pharmaceutical characteristics. This review summarizes the published data about effects of imiquimod on various intracellular biochemical processes and signaling pathways.

Original Russian Text © S.V. Bozrova, V.A. Levitsky, S.A. Nedospasov, M.S. Drutskaya, 2013, published in Biomeditsinskaya Khimiya.