What question did this study set out to answer?

To review the biological challenges of targeting the c-Myc oncoprotein and evaluate emerging therapeutic strategies to translate direct c-Myc inhibitors into clinical practice.

January 4, 2021Molecular CancerOpen Access

Taking the Myc out of cancer: toward therapeutic strategies to directly inhibit c-Myc

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Authors

SMSarah K. MaddenUniversity of Cambridge AAAline D. de AraujoThe University of Queensland MGMara GerhardtUniversity of Bath

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Implication

Expert review reveals pathways for directly inhibiting c-Myc in cancer models, highlighting strategies like Omomyc miniaturization to enable clinical translation.

Key Points

To review the biological challenges of targeting the c-Myc oncoprotein and evaluate emerging therapeutic strategies to translate direct c-Myc inhibitors into clinical practice.
Literature review evaluating historical c-Myc inhibition attempts and lessons learned from existing small molecules and dominant-negative constructs.
Structural and mechanistic evaluation of novel modalities, focusing on the miniaturisation of the Omomyc peptide and the disruption of E-box DNA binding.
Direct c-Myc inhibition achieves rapid tumor regression in preclinical murine models while producing only mild, transient, and fully reversible side effects.
Miniaturized Omomyc derivatives and agents preventing basic helix-loop-helix transcription factor binding to E-box DNA elements present feasible routes to overcome historical undruggability.

Cite This Study

Madden et al. (2021) studied this question.

synapsesocial.com/papers/69dac16a387cf706986879fa https://doi.org/10.1186/s12943-020-01291-6

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Implication

Expert review reveals pathways for directly inhibiting c-Myc in cancer models, highlighting strategies like Omomyc miniaturization to enable clinical translation.

Taking the Myc out of cancer: toward therapeutic strategies to directly inhibit c-Myc

Discussion

Member takes

Implication

Key Points

Cite This Study

Taking the Myc out of cancer: toward therapeutic strategies to directly inhibit c-Myc

Discussion

Member takes

Implication

Key Points

Cite This Study

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