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Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance

Nature communications, 2016-04, Vol.7 (1), p.11384-11384, Article 11384

2016

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Conserved RNA-binding specificity of polycomb repressive complex 2 is achieved by dispersed amino acid patches in EZH2

eLife, 2017-11, Vol.6

2017

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Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial

Molecular cancer therapeutics, 2007-03, Vol.6 (3), p.945-956

2007

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Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497)

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.650-665

2018

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Structure of HIV-1 Reverse Transcriptase with the Inhibitor β-Thujaplicinol Bound at the RNase H Active Site

Structure (London), 2009-12, Vol.17 (12), p.1625-1635

2009

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SAH derived potent and selective EZH2 inhibitors

Bioorganic & medicinal chemistry letters, 2015-04, Vol.25 (7), p.1532-1537

2015

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Characterization of Specific N -α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library

ACS medicinal chemistry letters, 2020-06, Vol.11 (6), p.1175-1184

2020

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Comparison of a High-Throughput Mass Spectrometry Method and Radioactive Filter Binding to Assay the Protein Methyltransferase PRMT5

Assay and drug development technologies, 2015-05, Vol.13 (4), p.235-240

2015

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Tricyclic Benzimidazoles as Potent Poly(ADP-ribose) Polymerase-1 Inhibitors

Journal of medicinal chemistry, 2003-01, Vol.46 (2), p.210-213

2003

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The Crystal Structure of the RNA-Dependent RNA Polymerase from Human Rhinovirus: A Dual Function Target for Common Cold Antiviral Therapy

Structure (London), 2004-08, Vol.12 (8), p.1533-1544

2004

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Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone

Bioorganic & medicinal chemistry, 2008-12, Vol.18 (23), p.6273-6278

2008

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Ras-Catalyzed Hydrolysis of GTP: A New Perspective from Model Studies

Proceedings of the National Academy of Sciences - PNAS, 1996-08, Vol.93 (16), p.8160-8166

1996

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Novel Tricyclic Poly(ADP-ribose) Polymerase-1 Inhibitors with Potent Anticancer Chemopotentiating Activity: Design, Synthesis, and X-ray Cocrystal Structure

Journal of medicinal chemistry, 2002-11, Vol.45 (23), p.4961-4974

2002

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Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors

Bioorganic & medicinal chemistry letters, 2004-05, Vol.14 (10), p.2433-2437

2004

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A fluorescence polarization assay for screening inhibitors against the ribonuclease H activity of HIV-1 reverse transcriptase

Analytical biochemistry, 2006-04, Vol.351 (2), p.260-265

2006

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Design, Synthesis, and Evaluation of 3,4-Dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as Inhibitors of Poly(ADP-Ribose) Polymerase

Journal of medicinal chemistry, 2004-10, Vol.47 (22), p.5467-5481

2004

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Design, synthesis, and biological evaluation of novel human 5′-deoxy-5′-methylthioadenosine phosphorylase (MTAP) substrates

Bioorganic & medicinal chemistry letters, 2005-06, Vol.15 (11), p.2829-2833

2005

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Structural and functional analysis of EcoRI DNA methyltransferase by proteolysis

Biochemistry (Easton), 1991-03, Vol.30 (11), p.2940-2946

1991

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Structure of HIV-1 Reverse Transcriptase with the Inhibitor b-Thujaplicinol Bound at the RNase H Active Site

Structure (London), 2009-12, Vol.17 (12), p.1625-1635

2009

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Spectroscopic studies of arsenic(III) binding to Escherichia coli RI methyltransferase and to two mutants, C223S and W183F

Biochemistry (Easton), 1992-11, Vol.31 (43), p.10438-10442

1992

Volltextzugriff (PDF)

Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)‑5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)‑one (PF-06821497)

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.650-665

2018

Volltextzugriff (PDF)

The Crystal Structure of the RNA-Dependent RNA Polymerase from Human Rhinovirus

Structure (London), 2004-08, Vol.12 (8), p.1533-1544

2004

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Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance

Conserved RNA-binding specificity of polycomb repressive complex 2 is achieved by dispersed amino acid patches in EZH2

Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial

SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance

Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)‑ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors

Structure of HIV-1 Reverse Transcriptase with the Inhibitor β-Thujaplicinol Bound at the RNase H Active Site

SAH derived potent and selective EZH2 inhibitors

Characterization of Specific N -α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library

Comparison of a High-Throughput Mass Spectrometry Method and Radioactive Filter Binding to Assay the Protein Methyltransferase PRMT5

Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)‑ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors

Tricyclic Benzimidazoles as Potent Poly(ADP-ribose) Polymerase-1 Inhibitors

The Crystal Structure of the RNA-Dependent RNA Polymerase from Human Rhinovirus: A Dual Function Target for Common Cold Antiviral Therapy

Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone

Ras-Catalyzed Hydrolysis of GTP: A New Perspective from Model Studies

Novel Tricyclic Poly(ADP-ribose) Polymerase-1 Inhibitors with Potent Anticancer Chemopotentiating Activity: Design, Synthesis, and X-ray Cocrystal Structure

Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors

A fluorescence polarization assay for screening inhibitors against the ribonuclease H activity of HIV-1 reverse transcriptase

Design, Synthesis, and Evaluation of 3,4-Dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as Inhibitors of Poly(ADP-Ribose) Polymerase

Design, synthesis, and biological evaluation of novel human 5′-deoxy-5′-methylthioadenosine phosphorylase (MTAP) substrates

Structural and functional analysis of EcoRI DNA methyltransferase by proteolysis

Structure of HIV-1 Reverse Transcriptase with the Inhibitor b-Thujaplicinol Bound at the RNase H Active Site

Spectroscopic studies of arsenic(III) binding to Escherichia coli RI methyltransferase and to two mutants, C223S and W183F

The Crystal Structure of the RNA-Dependent RNA Polymerase from Human Rhinovirus

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