Targeting of Myc-Max dimerization for the treatment of cancer

DESCRIPTION (provided by applicant): Myc is a key transcriptional regulator due to its critical role in many fundamental cellular processes, such as cell cycle progression and cell growth. Therefore, dysregulation of Myc expression can lead to disease, including cancer. Myc is overexpressed in many human tumors, and it is estimated that 1 in 7 cancer deaths in the United States are resultant of high levels of this oncoprotein. Myc cannot act alone, however, and its oncogenic activity is dependent on heterodimerization with Max. Together, these basic helix-loop-helix leucine zipper (bHLHLZ) proteins interact via a protein-protein interaction (PPI). Notably, a single amino acid substitution within the Myc-Max interaction domain can prevent dimerization. Thus,minor perturbation in the dimer surface can profoundly affect the ability of Myc and Max to interact. This fact strongly supports the idea that it may be possible to identify small molecule inhibitors of the Myc-Max PPI. Sorrento Therapeutics' academ