Conference Proceedings
In vitro on-target and selectivity profiling of small-molecule inhibitors of the Myc/Max heterodimeric complex
Sang-Kyu Kim, Richard C Foitzik, Songhui Li, Andrew Vinson, Alex Shmaylov, Karen Jarvis, Susan James, Scott R Walker, Mark York, Benjamin Cao, Susan K Nilsson, Ricky W Johnstone
MOLECULAR CANCER THERAPEUTICS | AMER ASSOC CANCER RESEARCH | Published : 2019
Abstract
Abstract The expression and activity of the Myc oncoprotein is frequently dysregulated in human cancers due to Myc amplification, translocation, protein stabilization and/or convergence of oncogenic signaling pathways on Myc. Therapeutic inhibition of Myc is highly desirable however, prior efforts to identify specific and direct pharmacological inhibitors of Myc function have generally failed to yield Myc-selective drug-like small molecules. Herein, we have comprehensively profiled previously reported small molecule inhibitors of the Myc-Max heterodimeric complex (10058-F4, 10074-G5, MYCMI-6, KI-MS2-001/-008 (KI-MS2), Mycro3 & JKY-2-169), using an in vitro biological screening..
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