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Turning Up the Heat on MYC: Progress in Small-Molecule Inhibitors

Mihai I. Truica, Michael C. Burns, Huiying Han and Sarki A. Abdulkadir
Mihai I. Truica
1Department of Urology, Northwestern University Feinberg School of Medicine, Chicago, Illinois.
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Michael C. Burns
2Department of Hematology-Oncology, Northwestern University Feinberg School of Medicine, Chicago, Illinois.
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Huiying Han
1Department of Urology, Northwestern University Feinberg School of Medicine, Chicago, Illinois.
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Sarki A. Abdulkadir
1Department of Urology, Northwestern University Feinberg School of Medicine, Chicago, Illinois.
3The Robert H. Lurie Comprehensive Cancer Center, Northwestern University Feinberg School of Medicine, Chicago, Illinois.
4Department of Pathology, Northwestern University Feinberg School of Medicine, Chicago, Illinois.
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  • For correspondence: sarki.abdulkadir@northwestern.edu
DOI: 10.1158/0008-5472.CAN-20-2959 Published January 2021
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Abstract

MYC is a highly validated oncogenic transcription factor and cancer target. However, the disordered nature of this protein has made it a challenging target, with no clinical stage, direct small-molecule MYC inhibitors available. Recent work leveraging a large in silico chemical library and a rapid in vivo screen has expanded the chemotypes of direct small-molecule inhibitors (MYCi). Novel MYCi represent a class of improved MYC chemical probes that bind directly to MYC to inhibit its function and to promote its degradation by enhancing GSK3β–mediated phosphorylation. One of these compounds, MYCi975, has shown remarkable tolerability and efficacy in vivo and is associated with a selective effect on MYC target gene expression. Additional effects of MYCi on the tumor immune microenvironment including immune cell infiltration and upregulation of PD-L1 expression provide a rationale for combining MYCi with anti–PD-1/PD-L1 therapy to enhance antitumor efficacy. Our strategy for developing MYCi demonstrates an efficient way to identify selective and well-tolerated MYC inhibitors. The new MYCi provide tools for probing MYC function and serve as starting points for the development of novel anti-MYC therapeutics.

Footnotes

  • Cancer Res 2021;81:248–53

  • Received September 1, 2020.
  • Revision received October 1, 2020.
  • Accepted October 15, 2020.
  • Published first October 21, 2020.
  • ©2020 American Association for Cancer Research.
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Cancer Research: 81 (2)
January 2021
Volume 81, Issue 2
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Turning Up the Heat on MYC: Progress in Small-Molecule Inhibitors
Mihai I. Truica, Michael C. Burns, Huiying Han and Sarki A. Abdulkadir
Cancer Res January 15 2021 (81) (2) 248-253; DOI: 10.1158/0008-5472.CAN-20-2959

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Turning Up the Heat on MYC: Progress in Small-Molecule Inhibitors
Mihai I. Truica, Michael C. Burns, Huiying Han and Sarki A. Abdulkadir
Cancer Res January 15 2021 (81) (2) 248-253; DOI: 10.1158/0008-5472.CAN-20-2959
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  • Article
    • Abstract
    • Introduction
    • The Enduring Challenge of Drugging the “Undruggable”
    • Blocking and Degrading MYC
    • A Therapeutic Window for MYC Inhibition
    • MYCi Remodeling of the Tumor Immune Microenvironment and Therapeutic Implications
    • Perspective
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