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2016 ; 5
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Strategically targeting MYC in cancer
#MMPMID27081479
Posternak V
; Cole MD
F1000Res
2016[]; 5
(ä): ä PMID27081479
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MYC is a major driver of cancer cell growth and mediates a transcriptional
program spanning cell growth, the cell cycle, metabolism, and cell survival. Many
efforts have been made to deliberately target MYC for cancer therapy. A variety
of compounds have been generated to inhibit MYC function or stability, either
directly or indirectly. The most direct inhibitors target the interaction between
MYC and MAX, which is required for DNA binding. Unfortunately, these compounds do
not have the desired pharmacokinetics and pharmacodynamics for in vivo
application. Recent studies report the indirect inhibition of MYC through the
development of two compounds, JQ1 and THZ1, which target factors involved in
unique stages of transcription. These compounds appear to have significant
therapeutic value for cancers with high levels of MYC, although some effects are
MYC-independent. These approaches serve as a foundation for developing novel
compounds to pharmacologically target MYC-driven cancers.
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