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. 2021 Oct 21;13(1):39–53. doi: 10.1039/d1md00274k

The inhibitors targeting the bottom pocket of the EED protein and their related research.

Compound Sequence or structure Selectivity and binding Associated tumor type Publication year Ref.
SAH-EZH2 FSSNRXKILXRTEILNQEWKQRRIQPV (1) Selective inhibition for PRC2 (1) DLBCL with EZH2 mutations: Karpas422, Pfeiffer 2014 69
(2) Binding to EED with KD = 0.32 nM (2) Breast cancer: MDA-MB-231
(3) Prostate cancer: DU145
(4) Leukemia: MLL-AF9
Astemizole graphic file with name d1md00274k-u7.jpg (1) Selective inhibition for PRC2 DLBCL containing EZH2 mutations and WT EZH2: SU-DHL4, SU-DHL6, DB, Pfeiffer; Toledo 2014 72
(2) Binding to EED with ΔTm >4 °C
Wedelolactone graphic file with name d1md00274k-u8.jpg Binding to EED with KD = 2.82 μM (1) Hepatocellular lines HepG2 2015 77
(2) Monocytic leukemia cells THP1
(3) Myeloid leukemia cells K562
DC-PRC2in-01 graphic file with name d1md00274k-u9.jpg (1) Selective inhibition for PRC2 DLBCL with EZH2 mutations: SU-DHL4, DB, Pfeiffer, Karpas422 2021 73
(2) Binding to EED with KD = 4.56 μM