Therapeutic targeting of "undruggable" MYC

Area of Science:

• Oncology
• Molecular Biology
• Drug Discovery

Background:

• The MYC oncoprotein is a critical regulator of cell proliferation, differentiation, and apoptosis.
• Dysregulation of MYC is observed in approximately 70% of human cancers, contributing to tumor initiation and progression.

Purpose of the Study:

• To review the functional and structural characteristics of the MYC protein.
• To provide an overview of MYC interactors that modulate its oncogenic activity.
• To summarize therapeutic strategies targeting MYC, including direct and indirect inhibition approaches.

Main Methods:

• Literature review of MYC's role in cancer.
• Analysis of MYC protein structure and function.
• Overview of identified MYC interactors.
• Summary of current and emerging MYC-targeting therapeutic strategies.

Main Results:

• MYC controls fundamental cellular processes and its aberrant expression is a hallmark of many cancers.
• In vivo studies demonstrate that MYC inhibition leads to significant anti-proliferative effects and tumor regression.
• Targeting MYC presents a promising therapeutic window due to reversible effects on healthy tissues.

Conclusions:

• MYC is a highly attractive therapeutic target for cancer treatment due to its central role in oncogenesis and the potential for selective inhibition.
• Understanding MYC's interactome is crucial for developing effective strategies to abrogate its oncogenic functions.
• Various approaches are being developed to directly or indirectly target MYC, offering new avenues for cancer drug development.