Abstract
Myc is a transcription factor driving growth and proliferation of cells and involved in the majority of human tumors. Despite a huge body of literature on this critical oncogene, our understanding of the exact molecular determinants and mechanisms that underlie its function is still surprisingly limited. Indubitably though, its crucial and non-redundant role in cancer biology makes it an attractive target. However, achieving successful clinical Myc inhibition has proven challenging so far, as this nuclear protein is an intrinsically disordered polypeptide devoid of any classical ligand binding pockets. Indeed, Myc only adopts a (partially) folded structure in some contexts and upon interacting with some protein partners, for instance when dimerizing with MAX to bind DNA. Here, we review the cumulative knowledge on Myc structure and biophysics and discuss the implications for its biological function and the development of improved Myc inhibitors. We focus this biophysical walkthrough mainly on the basic region helix–loop–helix leucine zipper motif (bHLHLZ), as it has been the principal target for inhibitory approaches so far.
Highlights
The MYC transcription factor regulates the expression of genes controlling the growth and proliferation of cells
We focus this biophysical walkthrough mainly on the basic region helix–loop–helix leucine zipper motif, as it has been the principal target for inhibitory approaches so far
(L-Myc) identified in lung cancer samples [6,7]. Both were later found to be expressed in many additional tissues and tumor types, and the nuclear localization was confirmed for the all Myc family protein members (MYC, MYCL, and MYCN, on Myc)
Summary
The MYC transcription factor ( known as c-Myc) regulates the expression of genes controlling the growth and proliferation of cells. Of Myc-activated target by recruiting corepressor complexes We summarize demonstration of the relevance of Myc asunveiled therapeutic target in cancer has provided significant structural and biophysical data that have distinctive features of Myc biology and some hints to overcome technical hurdles to identify potent and specific inhibitors [20]. In this review, they drive provide to targetthe it more efficiently. We summarize the structural and biophysical data that have unveiled distinctive features of Myc biology and some hints they to target it more of efficiently
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