Feb 19, 2025 · This Review provides an overview of the various strategies to inhibit MYC, focusing on the most recently described inhibitors and those that have reached clinical trials.

In vivo studies show that MYC inhibition elicits a prominent anti-proliferative effect and sustained tumor regression while any alteration on healthy tissue remains reversible. This opens an exploitable window for treatment that makes MYC one of the most appealing therapeutic targets for cancer drug development.

Nov 11, 2019 · We developed a series of small-molecule MYC inhibitors that engage MYC inside cells, disrupt MYC/MAX dimers, and impair MYC-driven gene expression. The compounds enhance MYC phosphorylation on threonine-58, consequently increasing proteasome-mediated MYC degradation.

Apr 29, 2022 · Our results demonstrate that MYCi975 selectively inhibits MYC target gene expression and provide a mechanistic rationale for potential combination therapies. MYC regulates multiple gene programs, raising questions about the potential selectivity and downstream transcriptional consequences of MYC inhibitors as cancer therapeutics.

Mar 10, 2021 · Silvestrol, an inhibitor of the eIF4A helicase, suppresses the Myc protein levels without influencing MYC mRNA levels in SW480 cells. 41 It also inhibits tumor growth in a mouse model of ...

Developing a clinical inhibitor for Myc has been particularly challenging owing to its intrinsically disordered nature and lack of a binding pocket, coupled with concerns regarding potentially deleterious side effects in normal proliferating tissues.

Here we have given a concise overview of the strategies employed to inhibit Myc to date, with a particular focus on their applicability in clinical practice. Direct inhibition of Myc expression Direct Myc inhibition can be achieved either by interference with its production or function.

Aug 2, 2021 · Developing a clinical inhibitor for Myc has been particularly challenging owing to its intrinsically disordered nature and lack of a binding pocket, coupled with concerns regarding potentially deleterious side effects in normal proliferating tissues.

Aug 25, 2021 · In vivo studies show that MYC inhibition elicits a prominent anti-proliferative effect and sustained tumor regression while any alteration on healthy tissue remains reversible. This opens an exploitable window for treatment that makes MYC one of the most appealing therapeutic targets for cancer drug development.

Mar 25, 2023 · How MYC inhibits immune cells and promotes tumor escape in the tumor microenvironment? What are the key molecules in the MYC pathway mediating antitumor immunity?