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Targeting Transcription Factors in Cancer: From “Undruggable” to “Druggable”

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Transcription Factor Regulatory Networks

Part of the book series: Methods in Molecular Biology ((MIMB,volume 2594))

Abstract

Deregulation of transcription factors is critical to hallmarks of cancer. Genetic mutations, gene fusions, amplifications or deletions, epigenetic alternations, and aberrant post-transcriptional modification of transcription factors are involved in the regulation of various stages of carcinogenesis, including cancer initiation, progression, and metastasis. Thus, targeting the dysfunctional transcription factors may lead to new cancer therapeutic strategies. However, transcription factors are conventionally considered as “undruggable.” Here, we summarize the recent progresses in understanding the regulation of transcription factors in cancers and strategies to target transcription factors and co-factors for preclinical and clinical drug development, particularly focusing on c-Myc, YAP/TAZ, and β-catenin due to their significance and interplays in cancer.

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Acknowledgments

The authors would like to thank Melanoma Research Alliance (MRA)-Samuel M. Fisher Memorial Established Investigator award and NIH R01s (5R01DK107651 and 1R01CA238270-01) for the support of our work. The figures are created with BioRender.com.

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  1. Cutaneous Biology Research Center, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA, USA

    Zhipeng Tao & Xu Wu

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  1. Zhipeng Tao
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  2. Xu Wu
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Correspondence to Zhipeng Tao or Xu Wu .

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  1. Computational Biology Department, Carnegie Mellon University, Pittsburgh, PA, USA

    Qi Song

  2. Cutaneous Biology Research Center, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA, USA

    Zhipeng Tao

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Tao, Z., Wu, X. (2023). Targeting Transcription Factors in Cancer: From “Undruggable” to “Druggable”. In: Song, Q., Tao, Z. (eds) Transcription Factor Regulatory Networks. Methods in Molecular Biology, vol 2594. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-2815-7_9

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  • DOI: https://doi.org/10.1007/978-1-0716-2815-7_9

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