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Omics · study · 2026

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

Listed in NCBI GEO

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.

Description

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.

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Life Sciences
Inferred from text
Cancer 75% · Genetics 68% · RNA sequencing 65%
Provenance · 1 source records, 10 field assertions
SourceKeyLast seenRaw
NCBI GEOGSE28157015 d agoJSON v1
FieldAssertionExtractorEvidence
access_levelsource · NCBI GEOconnector:ncbi_geo@1.0.0
concepts[disease].local:disease:cancerenrichment · NCBI GEOkeyword-concept-rules@1.0.0title+description (75%)
concepts[field].anzsrc:group:3105enrichment · NCBI GEOtaxonomy-embedding@1.1.0title+keywords+description (68%)
concepts[field].local:field:life-sciencesmapping · NCBI GEOconnector:ncbi_geo@1.0.0
concepts[method].geo_series_type:expression-profiling-by-high-throughput-sequencingsource · NCBI GEOconnector:ncbi_geo@1.0.0/gdstype
concepts[modality].local:modality:rna-seqenrichment · NCBI GEOkeyword-concept-rules@1.0.0title+description (65%)
concepts[organism].NCBITaxon:9606source · NCBI GEOconnector:ncbi_geo@1.0.0/taxon
descriptionsource · NCBI GEOconnector:ncbi_geo@1.0.0/summary
publication_datesource · NCBI GEOconnector:ncbi_geo@1.0.0
titlesource · NCBI GEOconnector:ncbi_geo@1.0.0/title