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PRC2 and SWI/SNF Chromatin Remodeling Complexes in Health and Disease

Biochemistry (Easton), 2016-03, Vol.55 (11), p.1600-1614

2016

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Molecular Pathways: Protein Methyltransferases in Cancer

Clinical cancer research, 2013-12, Vol.19 (23), p.6344-6350

COPELAND, Robert A

2013

Volltextzugriff (PDF)

Residence Time of Receptor−Ligand Complexes and Its Effect on Biological Function

Biochemistry (Easton), 2008-05, Vol.47 (20), p.5481-5492

2008

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The drug-target residence time model: a 10-year retrospective

Nature reviews. Drug discovery, 2016-02, Vol.15 (2), p.87-95

Copeland, Robert A

2016

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Drug Discovery and Chemical Biology of Cancer Epigenetics

Cell chemical biology, 2017-09, Vol.24 (9), p.1120-1147

2017

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Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

Proceedings of the National Academy of Sciences - PNAS, 2013-05, Vol.110 (19), p.7922-7927

2013

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Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas

Proceedings of the National Academy of Sciences - PNAS, 2010-12, Vol.107 (49), p.20980-20985

2010

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Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

Blood, 2013-08, Vol.122 (6), p.1017-1025

2013

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Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma

Molecular cancer therapeutics, 2014-04, Vol.13 (4), p.842-854

2014

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A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

Nature chemical biology, 2012-11, Vol.8 (11), p.890

2012

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Selective Killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models

Molecular cancer therapeutics, 2017-05, Vol.16 (5), p.850-860

2017

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The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat

Journal of medicinal chemistry, 2016-02, Vol.59 (4), p.1556-1564

2016

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Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma

PloS one, 2016-07, Vol.11 (7), p.e0158888-e0158888

2016

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Impact of enzyme concentration and residence time on apparent activity recovery in jump dilution analysis

Analytical biochemistry, 2011-09, Vol.416 (2), p.206-210

2011

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EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL

Molecular cancer therapeutics, 2017-11, Vol.16 (11), p.2586-2597

2017

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Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas

PloS one, 2014-12, Vol.9 (12), p.e111840

2014

Volltextzugriff (PDF)

Epigallocatechin gallate (EGCG), a major component of green tea, is a dual phosphoinositide-3-kinase/mTOR inhibitor

Biochemical and biophysical research communications, 2011-03, Vol.406 (2), p.194-199

2011

Volltextzugriff (PDF)

Targeting epigenetic regulators for cancer therapy

Annals of the New York Academy of Sciences, 2014-02, Vol.1309 (1), p.30-36

2014

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A687V EZH2 is a gain-of-function mutation found in lymphoma patients

FEBS letters, 2012-09, Vol.586 (19), p.3448-3451

2012

Volltextzugriff (PDF)

Chemogenetic Analysis of Human Protein Methyltransferases

Chemical biology & drug design, 2011-08, Vol.78 (2), p.199-210

2011

Volltextzugriff (PDF)

Protein methyltransferase inhibitors as precision cancer therapeutics: a decade of discovery

Philosophical transactions of the Royal Society of London. Series B. Biological sciences, 2018-06, Vol.373 (1748)

Copeland, Robert A

2018

Volltextzugriff (PDF)

Evaluation of enzyme inhibitors in drug discovery: a guide for medicinal chemists and pharmacologists, second edition

Copeland, Robert A

2nd ed., 2013

Volltextzugriff (PDF)

Identification of a peptide inhibitor for the histone methyltransferase WHSC1

PloS one, 2018-05, Vol.13 (5), p.e0197082-e0197082

2018

Volltextzugriff (PDF)

The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states

FEBS letters, 2011-10, Vol.585 (19), p.3011-3014

2011

Volltextzugriff (PDF)

Evolution of the drug-target residence time model

Expert opinion on drug discovery, 2021-12, Vol.16 (12), p.1441-1451

Copeland, Robert A.

2021

Volltextzugriff (PDF)

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PRC2 and SWI/SNF Chromatin Remodeling Complexes in Health and Disease

Molecular Pathways: Protein Methyltransferases in Cancer

Residence Time of Receptor−Ligand Complexes and Its Effect on Biological Function

The drug-target residence time model: a 10-year retrospective

Drug Discovery and Chemical Biology of Cancer Epigenetics

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

Selective Killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat

Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma

Impact of enzyme concentration and residence time on apparent activity recovery in jump dilution analysis

EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL

Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas

Epigallocatechin gallate (EGCG), a major component of green tea, is a dual phosphoinositide-3-kinase/mTOR inhibitor

Targeting epigenetic regulators for cancer therapy

A687V EZH2 is a gain-of-function mutation found in lymphoma patients

Chemogenetic Analysis of Human Protein Methyltransferases

Protein methyltransferase inhibitors as precision cancer therapeutics: a decade of discovery

Evaluation of enzyme inhibitors in drug discovery: a guide for medicinal chemists and pharmacologists, second edition

Identification of a peptide inhibitor for the histone methyltransferase WHSC1

The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states

Evolution of the drug-target residence time model

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