Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L
about
Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectivesTargeting histone methyltransferases and demethylases in clinical trials for cancer therapyPotent inhibition of DOT1L as treatment of MLL-fusion leukemiaThe high-resolution crystal structure of phosphatidylinositol 4-kinase IIβ and the crystal structure of phosphatidylinositol 4-kinase IIα containing a nucleoside analogue provide a structural basis for isoform-specific inhibitor designHistone lysine methyltransferases as anti-cancer targets for drug discoveryDiscovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8DOT1L inhibition sensitizes MLL-rearranged AML to chemotherapyDiscovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation ApproachA medicinal chemistry perspective for targeting histone H3 lysine-79 methyltransferase DOT1L.Chromatin proteins and modifications as drug targets.Small-molecular modulators of cancer-associated epigenetic mechanisms.Structure-activity relationship studies of SETD8 inhibitors.Inhibition of histone H3K79 methylation selectively inhibits proliferation, self-renewal and metastatic potential of breast cancerSelective inhibitors of protein methyltransferasesDOT1L inhibits SIRT1-mediated epigenetic silencing to maintain leukemic gene expression in MLL-rearranged leukemia.Structure-guided DOT1L probe optimization by label-free ligand displacement.Targeting DOT1L and HOX gene expression in MLL-rearranged leukemia and beyondMLL leukemia induction by genome editing of human CD34+ hematopoietic cells.The histone methyltransferase DOT1L: regulatory functions and a cancer therapy target.Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.3-(Piperidin-4-ylmethoxy)pyridine Containing Compounds Are Potent Inhibitors of Lysine Specific Demethylase 1.Synthesis, Activity and Metabolic Stability of Non-Ribose Containing Inhibitors of Histone Methyltransferase DOT1L.Targeted drug discovery for pediatric leukemia.DOT1L as a therapeutic target for the treatment of DNMT3A-mutant acute myeloid leukemiaDiscovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.Dynamics of DOT1L localization and H3K79 methylation during meiotic prophase I in mouse spermatocytes.SAM/SAH Analogs as Versatile Tools for SAM-Dependent Methyltransferases.Inhibitors of Protein Methyltransferases and Demethylases.Pharmacological inhibition of LSD1 for the treatment of MLL-rearranged leukemia.Inhibitors of enzymes catalyzing modifications to histone lysine residues: structure, function and activity.Applications of isothermal titration calorimetry - the research and technical developments from 2011 to 2015.Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket.Nucleophilic displacement reactions of 5'-derivatised nucleosides in a vibration ball mill.Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.Substituted purine and 7-deazapurine compounds as modulators of epigenetic enzymes: a patent evaluation (WO2012075381)
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P2860
Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L
description
2012 nî lūn-bûn
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2012年の論文
@ja
2012年学术文章
@wuu
2012年学术文章
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2012年学术文章
@zh-hans
2012年学术文章
@zh-my
2012年学术文章
@zh-sg
2012年學術文章
@yue
2012年學術文章
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2012年學術文章
@zh-hant
name
Synthesis and structure-activi ...... istone methyltransferase DOT1L
@ast
Synthesis and structure-activi ...... istone methyltransferase DOT1L
@en
type
label
Synthesis and structure-activi ...... istone methyltransferase DOT1L
@ast
Synthesis and structure-activi ...... istone methyltransferase DOT1L
@en
prefLabel
Synthesis and structure-activi ...... istone methyltransferase DOT1L
@ast
Synthesis and structure-activi ...... istone methyltransferase DOT1L
@en
P2093
P2860
P356
P1476
Synthesis and structure-activi ...... istone methyltransferase DOT1L
@en
P2093
Guobin Cai
Hong Jiang
Justin L Anglin
Lisheng Deng
Pinhong Chen
Yongcheng Song
P2860
P304
P356
10.1021/JM300917H
P407
P50
P577
2012-09-06T00:00:00Z