Search Results - "CHAN, Homan"
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An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED
Published in Nature chemical biology (01-04-2017)“…H3K27me3 binding to the EED pocket of the Polycomb repressive complex 2 (PRC2) is required to activate PRC2. An allosteric small-molecule inhibitor of PRC2 was…”
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Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation
Published in Proceedings of the National Academy of Sciences - PNAS (26-12-2012)“…Ezh2 (Enhancer of zeste homolog 2) protein is the enzymatic component of the Polycomb repressive complex 2 (PRC2), which represses gene expression by…”
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Histone Methylation by PRC2 Is Inhibited by Active Chromatin Marks
Published in Molecular cell (06-05-2011)“…The Polycomb repressive complex 2 (PRC2) confers transcriptional repression through histone H3 lysine 27 trimethylation (H3K27me3). Here, we examined how PRC2…”
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NSD2 Is Recruited through Its PHD Domain to Oncogenic Gene Loci to Drive Multiple Myeloma
Published in Cancer research (Chicago, Ill.) (15-10-2013)“…Histone lysine methyltransferase NSD2 (WHSC1/MMSET) is overexpressed frequently in multiple myeloma due to the t(4;14) translocation associated with 15% to 20%…”
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6‑Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors
Published in Journal of medicinal chemistry (28-02-2019)“…Protein tyrosine phosphatase SHP2 is an oncoprotein associated with cancer as well as a potential immune modulator because of its role in the programmed cell…”
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Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors
Published in Journal of medicinal chemistry (28-02-2019)“…SHP2 is a nonreceptor protein tyrosine phosphatase within the mitogen-activated protein kinase (MAPK) pathway controlling cell growth, differentiation, and…”
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A chemical genetics approach for the functional assessment of novel cancer genes
Published in Cancer research (Chicago, Ill.) (15-05-2015)“…Assessing the functional significance of novel putative oncogenes remains a significant challenge given the limitations of current loss-of-function tools…”
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Abstract LB-005: Allosteric SHP2 phosphatase inhibition: Multiple mechanisms and chemotypes
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Protein tyrosine phosphatase SHP2 is an oncoprotein associated with cancer as well as a potential immune modulator due to its role in the programmed cell death…”
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Correction to Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors
Published in Journal of medicinal chemistry (11-04-2019)Get full text
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Correction to 6‑Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors
Published in Journal of medicinal chemistry (11-04-2019)Get full text
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Abstract LB-288: An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED
Published in Cancer research (Chicago, Ill.) (01-07-2017)“…Polycomb repressive complex 2 (PRC2) consists of three core subunits, EZH2, EED and SUZ12 and plays pivotal roles in transcriptional regulation through its…”
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Abstract PR01: Global chromatin profiling identifies NSD2 mutations in pediatric acute lymphoblastic leukemia
Published in Cancer research (Chicago, Ill.) (01-07-2013)“…Epigenetic dysregulation is an emerging hallmark of cancers, and the identification of recurrent somatic mutations in chromatin modifying enzymes implies a…”
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