A novel inhibitor L755507 efficiently blocks c-Myc–MAX heterodimerization and induces apoptosis in cancer cells
Ashutosh Singh, Ankur Kumar, Prateek Kumar, Namyashree Nayak, Taniya Bhardwaj, Rajanish Giri, Neha Garg
Abstract
values. L755507 successfully disrupts the c-Myc-MAX heterodimer, resulting in decreased expression of c-Myc target genes. Spectroscopic and computational experiments demonstrated that L755507 binds to the c-Myc peptide and thereby stabilizes the helix-loop-helix conformation of the c-Myc transcription factor. Taken together, this study suggests that L755507 effectively inhibits the c-Myc-MAX heterodimerization and may be used for further optimization to develop a c-Myc-targeted antineoplastic drug.
Topics & Concepts
Transcription factorProto-Oncogene Proteins c-mycCancer cellCancer researchGeneDrug discoveryChemistryApoptosisBiologyTranscription (linguistics)Small moleculeCell biologyCancerBiochemistryGeneticsLinguisticsPhilosophyPeptidase Inhibition and AnalysisProtein Degradation and InhibitorsUbiquitin and proteasome pathways