FIGURE 3 from A Novel Class of Ribosome Modulating Agents Exploits Cancer Ribosome Heterogeneity to Selectively Target the CMS2 Subtype of Colorectal Cancer

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posted on 2023-06-05, 14:20 authored by Esteban Terzo, Shruti A. Apte, Simran Padhye, Saleh Rashed, Wesley Austin, Michael Caponegro, Anupama Reddy, Shuhao Shi, Christy Wang, Roger B. Clark, David Sidransky, Vijay Modur, Vasudeo Badarinarayana

ZKN-157 treatment results in cell-cycle arrest in a sensitive colorectal cancer cell line. A, Immunoblots for p21 following 24-hour treatments with DMSO or ZKN-157 (40 μmol/L) are shown. Bar graphs show quantitated intensities normalized to B2M (loading control). B, Bar graph plotting percentage of SW1417 cells from cell-cycle phases.

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ARTICLE ABSTRACT

This study demonstrates that ribosome heterogeneity in cancer can be exploited to develop selective ribogenesis inhibitors. The colorectal cancer CMS2 subtype, with a high unmet need for therapeutics, shows vulnerability to our novel selective ribosome modulator. The mechanism suggests that other cancer subtypes with high MYC activation could also be targeted.

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Keywords

Small Molecule Agents Gastrointestinal Cancers Colorectal cancer Chemistry & Chemical Biology Drug Targets

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CC BY