MAX Binders Targeting Disordered Myc Protein
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Solution Overview
Problem
The Myc protein is difficult to target using small molecule probes due to its disordered conformational structure, making it challenging to find specific probes for cancer treatment, and existing methods struggle to effectively inhibit its transcriptional activity in malignant cells.
Innovation Solution
Development of compounds that bind to MAX, thereby indirectly targeting Myc by modulating its transcriptional activity, including inhibitors of Myc, Mad, or Mxi1, to treat cancers and proliferative diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If small molecule probes are used to target Myc, then direct inhibition of Myc is achieved, but the disordered conformational structure of Myc makes it difficult to find specific probes
Solution Approach 1:
The patent uses MAX as an intermediary target instead of directly targeting Myc. Small molecule probes bind to MAX, which then indirectly inhibits Myc transcriptional activity. This approach overcomes the difficulty of finding specific probes for Myc's disordered structure while maintaining reliable Myc inhibition through the MAX-Myc interaction pathway
2Reliability
If compounds bind to MAX to indirectly target Myc, then Myc transcriptional activity is inhibited, but the complexity of the Myc-MAX interaction system increases
Solution Approach 1:
The patent extracts and targets a specific component (MAX) from the complex Myc-MAX interaction system. By focusing on MAX as the binding target rather than attempting to manage the entire Myc-MAX network, the approach simplifies the therapeutic strategy while maintaining effective Myc inhibition through the extracted MAX target
Data Source
AI summary
The present disclosure provides compounds of Formula (I′), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.