Functional inhibition of c-Myc using novel inhibitors identified through "hot spot" targeting.

ABSTRACT: Protein-protein interactions drive various biological processes in healthy as well as disease states. The transcription factor c-Myc plays a crucial role in maintaining cellular homeostasis, and its deregulated expression is linked to various human cancers; therefore, it can be considered a viable target for cancer therapeutics. However, the structural heterogeneity of c-Myc due to its disordered nature poses a major challenge to drug discovery. In the present study, we used an in silico alanine scanning mutagenesis approach to identify "hot spot" residues within the c-Myc/Myc-associated factor X interface, which is highly disordered and has not yet been systematically analyzed for potential small molecule binding sites. We then used the information gained from this analysis to screen pote

SUBMITTER: Singh A 

PROVIDER: S-EPMC9065629 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature