2020
DOI: 10.1080/07391102.2019.1711187
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Computer-aided screening for suppressor of variegation 4-20 homolog 1 inhibitors and their preliminary activity validation in human osteosarcoma

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Cited by 4 publications
(3 citation statements)
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“…Starting from the Specs subset of the ZINC database, containing over 200 000 compounds, 97 ( ZINC08398384 ) and 98 ( ZINC08439608 ) were selected and showed an inhibitory effect similar to the known inhibitor 96 , effectively reducing the expression level of dimethylated H4K20 in U2OS (at 1.25 and 2.5 μM, respectively) and attenuating the migration of osteosarcoma cells in vitro . 250…”
Section: Introductionmentioning
confidence: 99%
“…Starting from the Specs subset of the ZINC database, containing over 200 000 compounds, 97 ( ZINC08398384 ) and 98 ( ZINC08439608 ) were selected and showed an inhibitory effect similar to the known inhibitor 96 , effectively reducing the expression level of dimethylated H4K20 in U2OS (at 1.25 and 2.5 μM, respectively) and attenuating the migration of osteosarcoma cells in vitro . 250…”
Section: Introductionmentioning
confidence: 99%
“…A-196 inhibited 53BP1 foci formation upon ionizing radiation and reduced NHEJ-mediated DNA-break repair [ 392 ]. The development of two other compounds that could markedly reduce H4K20me2 in a dose-dependent manner has been reported [ 393 ].…”
Section: Targeting the Chromatin Response To Dsb Dna Damagementioning
confidence: 99%
“…For example, Chen et al uncover the first selective inhibitor against the disruptor of telomeric silencing 1like (DOT1L) (Chen et al, 2016), the most studied non-SETcontaining methyltransferase that is responsible for the mono-, di-and trimethylation of lysine 79 of histone H3 -H3K79 (Feoli et al, 2022). Zheng et al reported the combination of highthroughput screening, SBVS, and molecular dynamics to identify computational hits against a histone methyltransferase (Zheng et al, 2021). Kong et al used SBVS to uncover astemizole as an inhibitor of EZH2/EED (Kong, et al, 2014).…”
Section: Introductionmentioning
confidence: 99%