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Cancer epigenetics drug discovery and development: the challenge of hitting the mark

The Journal of clinical investigation, 2014-01, Vol.124 (1), p.64-69

2014

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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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BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models

PloS one, 2013-08, Vol.8 (8), p.e72967

2013

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Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

Proceedings of the National Academy of Sciences - PNAS, 2012-02, Vol.109 (8), p.2989-2994

2012

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Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer

Oncotarget, 2013-12, Vol.4 (12), p.2419-2429

2013

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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

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Smyd3 regulates cancer cell phenotypes and catalyzes histone H4 lysine 5 methylation

Epigenetics, 2012-04, Vol.7 (4), p.340-343

2012

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Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

ACS medicinal chemistry letters, 2012-12, Vol.3 (12), p.1091-1096

2012

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Role of Histone-Modifying Enzymes and Their Complexes in Regulation of Chromatin Biology

Biochemistry (Easton), 2016-03, Vol.55 (11), p.1584-1599

2016

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A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation

Molecular cancer therapeutics, 2014-12, Vol.13 (12), p.3062-3073

2014

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Long Residence Time Inhibition of EZH2 in Activated Polycomb Repressive Complex 2

ACS chemical biology, 2014-03, Vol.9 (3), p.622-629

2014

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Small-Molecule Targets in Immuno-Oncology

Cell chemical biology, 2017-09, Vol.24 (9), p.1148-1160

2017

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Effects of oncogenic p110α subunit mutations on the lipid kinase activity of phosphoinositide 3-kinase

Biochemical journal, 2008-01, Vol.409 (2), p.519-524

2008

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SMYD3 links lysine methylation of MAP3K2 to Ras-driven cancer

Nature (London), 2014-06, Vol.510 (7504), p.283-287

2014

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C-terminal region of USP7/HAUSP is critical for deubiquitination activity and contains a second mdm2/p53 binding site

Archives of biochemistry and biophysics, 2010-11, Vol.503 (2), p.207-212

2010

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EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

Nature (London), 2012-12, Vol.492 (7427), p.108-112

2012

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MEK inhibitors overcome resistance to BET inhibition across a number of solid and hematologic cancers

Oncogenesis (New York, NY), 2018-04, Vol.7 (4), p.35-12, Article 35

2018

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A Biochemical Rationale for the Anticancer Effects of Hsp90 Inhibitors: Slow, Tight Binding Inhibition by Geldanamycin and Its Analogues

Proceedings of the National Academy of Sciences - PNAS, 2006-05, Vol.103 (20), p.7625-7630

2006

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Evidence for allosteric interactions of antagonist binding to the smoothened receptor

The Journal of pharmacology and experimental therapeutics, 2009-06, Vol.329 (3), p.995-1005

2009

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Biochemical characterization of human HIF hydroxylases using HIF protein substrates that contain all three hydroxylation sites

Biochemical journal, 2011-06, Vol.436 (2), p.363-369

2011

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Substrate-Based Design of the First Class of Angiotensin-Converting Enzyme-Related Carboxypeptidase (ACE2) Inhibitors

Journal of the American Chemical Society, 2002-10, Vol.124 (40), p.11852-11853

2002

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Control of NF-kB activity in human melanoma by bromodomain and extra-terminal protein inhibitor I-BET151

Pigment cell and melanoma research, 2014-11, Vol.27 (6), p.1126-1137

2014

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The catalytic role of INCENP in Aurora B activation and the kinetic mechanism of Aurora B/INCENP

Biochemical journal, 2009-01, Vol.417 (1), p.355-360

2009

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Cancer epigenetics drug discovery and development: the challenge of hitting the mark

The Journal of clinical investigation, 2014-03, Vol.124 (3), p.1419-1419

2014

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Cancer epigenetics drug discovery and development: the challenge of hitting the mark

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

BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer

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

Smyd3 regulates cancer cell phenotypes and catalyzes histone H4 lysine 5 methylation

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

Role of Histone-Modifying Enzymes and Their Complexes in Regulation of Chromatin Biology

A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation

Long Residence Time Inhibition of EZH2 in Activated Polycomb Repressive Complex 2

Small-Molecule Targets in Immuno-Oncology

Effects of oncogenic p110α subunit mutations on the lipid kinase activity of phosphoinositide 3-kinase

SMYD3 links lysine methylation of MAP3K2 to Ras-driven cancer

C-terminal region of USP7/HAUSP is critical for deubiquitination activity and contains a second mdm2/p53 binding site

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

MEK inhibitors overcome resistance to BET inhibition across a number of solid and hematologic cancers

A Biochemical Rationale for the Anticancer Effects of Hsp90 Inhibitors: Slow, Tight Binding Inhibition by Geldanamycin and Its Analogues

Evidence for allosteric interactions of antagonist binding to the smoothened receptor

Biochemical characterization of human HIF hydroxylases using HIF protein substrates that contain all three hydroxylation sites

Substrate-Based Design of the First Class of Angiotensin-Converting Enzyme-Related Carboxypeptidase (ACE2) Inhibitors

Control of NF-kB activity in human melanoma by bromodomain and extra-terminal protein inhibitor I-BET151

The catalytic role of INCENP in Aurora B activation and the kinetic mechanism of Aurora B/INCENP

Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin

Cancer epigenetics drug discovery and development: the challenge of hitting the mark

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