MYC modulators in cancer: a patent review

ABSTRACT

Introduction: The important role of MYC in tumorigenesis makes it particularly important to design MYC modulators. Over the past decade, researchers have raised a number of strategies for designing MYC modulators, some of which are already in clinical trials. This paper aims to review the patents of MYC modulators.

Areas covered: The important biological relevance of c-MYC and the regulation pathways related to c-MYC are briefly introduced. Base on that, the MYC modulators reported in published patents and references primarily for cancer treatment are outlined, highlighting the structures and biological activities.

Expert opinion: There has been a growing awareness of finding and designing MYC modulators as novel anticancer drugs over recent years. Patents involving the discovery, synthesis, and application of MYC modulators are particularly important for further development in this field. Although finding direct MYC inhibitors or binders is challenging, MYC cannot be simply defined as an undruggable target. There is still substantial evidence proving the concept that MYC modulators can benefit to the treatment of both human hematological malignancies and solid tumors. More efforts should be taken to improve the activity and specificity of MYC modulators.

KEYWORDS:

• Myc
• anticancer
• modulators
• mechanism
• therapeutic strategy

Article highlights

• c-MYC acts as a transcription factor and plays key role in tumorigenesis. Activated Myc gene is found in a wide range of human hematological malignancies and solid tumors. Thus, c-MYC is an important biomarker for cancers.

• Designing and developing MYC direct modulators is challenging, primarily because the MYC protein lacks a pocket or groove that can act as a binding site for modulators and has a short half-life. Interfering with the MYC transcription, blocking the protein–protein interaction (PPI) of MYC and its cofactors, and influencing on signaling pathways related to MYC seem to be feasible strategies for finding MYC modulators.

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Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was funded by the National Natural Science Foundation of China (grant 81673286 for TM Ou; grant 81330077 for ZS Huang), the Guangdong Provincial Science and Technology Development Special Foundation (Public Interest Research and Capacity Building) (grant 2016A020217006 for TM Ou), and Guangdong Provincial Key Laboratory of Construction Foundation (grant 2011A060901014).