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

Bozrova S.V.1, Levitsky V.A.2, Nedospasov S.A.1, Drutskaya M.S.1

1. Engelhardt Institute of Molecular Biology RAS; Department of Immunology, Biological Faculty, Lomonosov Moscow State University
2. Engelhardt Institute of Molecular Biology RAS; Oncology Department Johns Hopkins University School of Medicine
Section: Review
DOI: 10.18097/PBMC20135903249      PubMed Id: 23987065
Year: 2013  Volume: 59  Issue: 3  Pages: 249-266
Imidazoquinolins represent a new group of compounds that recently entered into clinical practice as anti-tumor and anti-viral immune modulators. They are low molecular weight synthetic guanosine-like molecules. Although imiquimod, the most widely used imidazoquinolin, is recommended for the treatment of several forms of skin cancer and papillomas, the molecular mechanisms of its action are not fully understood. In particular, imiquimod has been characterized as a specific agonist of Toll-like receptor 7 (TLR7) and is widely used in this capacity in a large number of experimental studies and clinical trials. However, detailed analysis of the published data with the use of imiquimod, suggests that its biological activity can not be explained only by interaction with TLR7. There are indications of a direct interaction of imiquimod with adenosine receptors and other molecules that regulate the synthesis of cyclic adenosine monophosphate. A detailed understanding of the biochemical basis of imiquimod immunomodulating and antitumor effect will increase its clinical effectiveness and accelerate the development of new drugs with similar but improved medical properties. This review summarizes the published data concerning the effects of imiquimod on a variety of intracellular biochemical processes and signaling pathways.
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Keywords: Imidazoqinolins, imiquimod, tumor necrosis factor, anti-inflammatory drug, cAMP

Bozrova, S. V., Levitsky, V. A., Nedospasov, S. A., Drutskaya, M. S. (2013). Imiquimod: the biochemical mechanisms of immunomodulatory and anti-inflammatory activity. Biomeditsinskaya Khimiya, 59(3), 249-266.
This paper is also available as the English translation: 10.1134/S1990750813020042
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