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Article
Assigning functionality to cysteines by base editing of cancer dependency genes
Covalent chemistry represents an attractive strategy for expanding the ligandability of the proteome, and chemical proteomics has revealed numerous electrophile-reactive cysteines on diverse human proteins. De...
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Article
Remodeling oncogenic transcriptomes by small molecules targeting NONO
Much of the human proteome is involved in mRNA homeostasis, but most RNA-binding proteins lack chemical probes. Here we identify electrophilic small molecules that rapidly and stereoselectively decrease the ex...
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Article
ABHD17 regulation of plasma membrane palmitoylation and N-Ras-dependent cancer growth
Multiple Ras proteins, including N-Ras, depend on a palmitoylation/depalmitoylation cycle to regulate their subcellular trafficking and oncogenicity. General lipase inhibitors such as Palmostatin M (Palm M) bl...
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Article
Expedited map** of the ligandable proteome using fully functionalized enantiomeric probe pairs
A fundamental challenge in chemical biology and medicine is to understand and expand the fraction of the human proteome that can be targeted by small molecules. We recently described a strategy that integrates...
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Article
Open AccessAn HDAC3-PROX1 corepressor module acts on HNF4α to control hepatic triglycerides
The histone deacetylase HDAC3 is a critical mediator of hepatic lipid metabolism, and liver-specific deletion of HDAC3 leads to fatty liver. To elucidate the underlying mechanism, here we report a method of cr...
