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Molecular and cellular toxicological profiling of DNA bis-intercalator, quinoxaline compounds: echinomycin as the versatile lead

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Abstract

Of quinoxaline compounds, echinomycin is classically known as an antitumor agent which binds to DNA via a mechanism of bis-intercalation. In addition to intercalation, quinoxaline compounds such as echinomycin, echinomycin derivatives or analogues might control anomalous cellular proliferation in eukaryotes via specifically triggering cellular signaling pathways in mitochondria, as well as under hypoxia. Further, since echinomycin was proven to be a specific inhibitor of HIF-1α, these novel mechanisms could be clinically applied in the development of therapeutics against cancer, infection, obesity, fibrosis, and autoimmune disease. Herein, this review focuses on the current toxicological profiles of echinomycin as well its potential applications in medicine.

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Authors and Affiliations

  1. Department of Microbiology and Institute for Clinical and Translational Research, Catholic Kwandong University College of Medicine, Gangneung, 25601, Republic of Korea

    Yoon-Sun Park & Woon-Seob Shin

  2. Department of Microbiology, Wonju College of Medicine, Yonsei University, Wonju, Gangwon, 26426, Republic of Korea

    Cheol-Su Kim & Soo-Ki Kim

  3. Institute of Genomic Cohort, Wonju College of Medicine, Yonsei University, Wonju, Gangwon, 26426, Republic of Korea

    Soo-Ki Kim

  4. Department of Basic Science, Wonju College of Medicine, Yonsei University, Wonju, Gangwon, 26426, Republic of Korea

    Chan Mug Ahn

  5. Key Laboratory for Regenerative Medicine of Ministry of Education, Ji Nan University, Guangzhou, 510632, People’s Republic of China

    Xu-Feng Qi

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  1. Yoon-Sun Park
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Correspondence to Soo-Ki Kim.

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Park, YS., Shin, WS., Kim, CS. et al. Molecular and cellular toxicological profiling of DNA bis-intercalator, quinoxaline compounds: echinomycin as the versatile lead. Mol. Cell. Toxicol. 14, 9–18 (2018). https://doi.org/10.1007/s13273-018-0002-8

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  • DOI: https://doi.org/10.1007/s13273-018-0002-8

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