102 (PB092) - First-in-class heterobifunctional proteomimetic polymer capable of direct inhibition of Myc and target it for degradation

Abstract

Background: The proto-oncogene Myc is known to play critical roles in tumorigenesis and therapeutic resistance, being dysregulated in up to 70% of all human cancers. Heterodimerization with its binding partner Max is required for oncogenic transformation, yet the development of small molecule inhibitors has been hampered due to the lack of suitable binding pockets. Myc inhibitory peptides derived from the first helix (H1) of the bHLH-LZ region have been developed in efforts to address this limitation.