Cellular experiments to study the inhibition of c-Myc/MAX heterodimerization.

The c-Myc oncogene is a master regulator of cancer cell metabolism, which controls a variety of pathways, including cell proliferation, cell cycle, apoptosis, and epigenetics. Belonging to the bHLH family of transcription factors, c-Myc forms a heterodimeric complex with another bHLH family protein MAX. c-Myc deregulation is reported in most cancers. This heterodimeric complex is a potent transcription factor that controls the expression of the target gene by binding to the E-box sequence and thereby controlling cancer cell proliferation. c-Myc in isolation has a partially folded structure and cannot carry the transcription. However, its heterodimerization provides the ability to bind DNA and carry out the regulatory function. Therefore, heterodimerization of c-Myc and Max is of great interest for cancers, and it has always been considered a target for cancer therapy. This book chapter will present a detailed protocol of cellular experiments employed to validate the in vitro potency of c-Myc inhibitor candidates to search for a novel c-Myc-targeted neoplastic drug.