The transcription factor Max is a basic-helix-loop-helix leucine zipper (bHLHLZ) protein that forms homodimers or interacts with other bHLHLZ proteins, including Myc and Mxd proteins. Among this dynamic network of interactions, the Myc/Max heterodimer has crucial roles in regulating normal cellular processes, but its transcriptional activity is deregulated in a majority of human cancers. Despite this significance, the arsenal of high-quality chemical probes to interrogate these proteins remains limited. We used small molecule microarrays to identify compounds that bind Max in a mechanistically unbiased manner. We discovered the asymmetric polycyclic lactam, KI-MS2-008, which stabilizes the Max homodimer while reducing Myc protein and Myc-regulated transcript levels. KI-MS2-008 also decreases viable cancer cell growth in a Myc-dependent manner and suppresses tumor growth in vivo. This approach demonstrates the feasibility of modulating Max with small molecules and supports altering Max dimerization as an alternative approach to targeting Myc.
Pubmed ID: 30880155 RIS Download
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View all literature mentionsSoftware for aligning sequencing reads against large reference genome. Consists of three algorithms: BWA-backtrack, BWA-SW and BWA-MEM. First for sequence reads up to 100bp, and other two for longer sequences ranged from 70bp to 1Mbp.
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View all literature mentionsThis unknown targets IgG (H+L)
View all literature mentionsThis polyclonal targets IgG
View all literature mentionsThis monoclonal targets Human MXD1
View all literature mentionsThis monoclonal targets Mono- and polyubiquitinylated conjugates mAb (FK2)
View all literature mentionsThis polyclonal secondary targets IgG (H+L)
View all literature mentionsThis polyclonal targets c-Myc (phospho T58) antibody
View all literature mentionsThis polyclonal targets IgG
View all literature mentionsThis polyclonal secondary targets IgG
View all literature mentionsThis polyclonal targets MAX
View all literature mentionsThis monoclonal targets Human c-Myc (phospho S62)
View all literature mentionsThis monoclonal targets c-Myc
View all literature mentionsThis polyclonal targets MYC
View all literature mentionsThis unknown targets normal rabbit IgG
View all literature mentionsThis monoclonal targets c-Myc
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View all literature mentionsThis polyclonal targets H3K27ac
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