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RNA-seq study using Karpas422 xenograft tumors after vehicle or PRC2 inhibitor C36 treatment

GSE281570 Homo sapiens Expression profiling by high throughput sequencing 6 samples Submitted 2026/06/23 Platform GPL24676
Summary
Polycomb Repressive Complex 2 (PRC2) is the conserved methyltransferase depositing mono-, di-, and tri- methylation (H3K27me1/me2/me3) on the lysine 27 of histone H3 and thereby represses gene transcription. EZH2 is the catalytic subunit of the histone methyltransferase Polycomb Repressive Complex 2 (PRC2), and EZH2 somatic gain-of-function (GoF) mutations are lymphoma-drivers. Therefore, EZH2/PRC2 is a critical target for cancer drug development. In the present study, we characterized a small molecule inhibitor of PRC2, C36, and demonstrated its novel allosteric inhibitory mechanism from biochemical and structural perspectives. C36 efficiently inhibits H3K27 trimethylation and specifically prevents the expression of PRC2 target genes in human tumor cell lines and xenograft tumor model. And through transcriptomic and proteomic studies critical pathways regulated by PRC2 inhibition were elucidated in B cell lymphoma.
Published in
Allosteric Inhibition of Polycomb Repressive Complex 2 by an EZH2-Selective Small Molecule Inhibitor
Cao T, Liu D, Gao H et al. · Advanced science (Weinheim, Baden-Wurttemberg, Germany) 2026 · PMID 42314051 · doi:10.1002/advs.76025
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Direct links to NCBI, no account and no request form: the whole study as GSE281570_RAW.tar, processed values as the series matrix, the supplementary file directory, and per-sample supplementary files for any of the 6 samples. Raw sequencing reads are also available from ENA.

Also filed as BioProject PRJNA1184741 and SRA study SRP544526. Searching any of these in the dataset finder brings you back here.

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