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Synonyms: E-7438 | EPZ 6438 | EPZ-6438 | EPZ6438 | Tazverik®
tazemetostat is an approved drug (FDA (2020))
Compound class: Synthetic organic
Comment: Tazemetostat is an oral, potent, first-in-class inhibitor of the histone methyltransferase, enhancer of zeste 2 polycomb repressive complex 2 subunit (EZH2) that was developed by Epizyme as anovel drug for the treatment of solid tumours and lymphomas with speciific genetic alterations. Link to Epizyme's tazemetostat webpage here.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
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Loss of INI1 expression is characteristic of both conventional and proximal-type epithelioid sarcoma.
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Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.
Proc Natl Acad Sci USA, 110 (19): 7922-7. [PMID:23620515]
3. Patil PA, Lombardo K, Sturtevant A, Mangray S, Yakirevich E. (2018)
Loss of Expression of a Novel Chromatin Remodeler SMARCA1 in Soft Tissue Sarcoma.
J Cytol Histol, 9 (6): 524. DOI: 10.4172/2157-7099.1000524 [PMID:31093468]