K. Kuntz

发表

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

Tim J. Wigle, R. Copeland, R. Pollock, 2013, Proceedings of the National Academy of Sciences.

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

Tim J. Wigle, Lei Jin, R. Copeland, 2011, FEBS letters.

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).

Brian J. Wilson, L. Shewchuk, P. Sabbatini, 2009, Bioorganic & medicinal chemistry letters.

Ti-Catalyzed Enantioselective Addition of Cyanide to Imines. A Practical Synthesis of Optically Pure α-Amino Acids

Clinton A. Krueger, M. Snapper, A. Hoveyda, 1999 .

Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.

L. Shewchuk, T. J. Lansing, R. Mook, 2008, Bioorganic & medicinal chemistry letters.

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

Tim J. Wigle, T. Riera, R. Copeland, 2016, ACS medicinal chemistry letters.

Regioselective synthesis of benzimidazole thiophene inhibitors of polo-like kinase 1

M. Cheung, J. Salovich, K. Hornberger, 2008 .

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity

Tim J. Wigle, R. Copeland, N. Waters, 2015, ACS medicinal chemistry letters.

Mechanism of enantioselective Ti-catalyzed Strecker reaction: peptide-based metal complexes as bifunctional catalysts.

M. Snapper, A. Hoveyda, K. Kuntz, 2001, Journal of the American Chemical Society.

Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule

Tim J. Wigle, M. Niepel, K. Swinger, 2021, Chembiochem : a European journal of chemical biology.

SEARCH FOR CHIRAL CATALYSTS THROUGH LIGAND DIVERSITY : SUBSTRATE-SPECIFIC CATALYSTS AND LIGAND SCREENING ON SOLID PHASE

K. Shimizu, Clinton A. Krueger, M. Snapper, 1997 .

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

Tim J. Wigle, E. Olhava, Lei Jin, 2012, Nature chemical biology.

277 The discovery and pre-clinical development of the first clinical stage EZH2-inhibitor, EPZ-6438 (E7438)

Tim J. Wigle, R. Copeland, R. Pollock, 2014 .

EZH2 Inhibitor EPZ-6438 Synergizes With Anti-Lymphoma Therapies In Preclinical Models

Tim J. Wigle, R. Copeland, R. Pollock, 2013 .

Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L

Tim J. Wigle, E. Olhava, Lei Jin, 2012, Chemical biology & drug design.

PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity.

Tim J. Wigle, M. Niepel, K. Swinger, 2021, Cancer cell.

Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma

Tim J. Wigle, Yonghong Xiao, R. Copeland, 2014, Molecular Cancer Therapeutics.

In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement.

M. Niepel, K. Swinger, A. Lu, 2020, Cell chemical biology.

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

R. Copeland, R. Pollock, V. Richon, 2016, Journal of medicinal chemistry.

Ti-Catalyzed Regio- and Enantioselective Synthesis of Unsaturated α-Amino Nitriles, Amides and Acids. Catalyst Identification Through Screening of Parallel Libraries.

M. Snapper, J. R. Porter, K. Kuntz, 2000 .

Ti-Catalyzed Regio- and Enantioselective Synthesis of Unsaturated α-Amino Nitriles, Amides, and Acids. Catalyst Identification through Screening of Parallel Libraries

James R. Porter, A. Hoveyda, J. R. Porter, 2000 .

Total synthesis of anti-HIV agent chloropeptin I.

M. Snapper, A. Hoveyda, K. Kuntz, 2003, Journal of the American Chemical Society.

Discovery of thiophene inhibitors of polo-like kinase.

D. Drewry, T. J. Lansing, R. Mook, 2009, Bioorganic & medicinal chemistry letters.

Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.

Yonghong Xiao, Jen-Chieh Tseng, Robert A Copeland, 2011, Cancer cell.

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

Lei Jin, R. Copeland, V. Richon, 2012, FEBS letters.

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

R. Copeland, R. Pollock, V. Richon, 2010, Proceedings of the National Academy of Sciences.

Histone Methyltransferases: Opportunities in Cancer Drug Discovery

V. Richon, R. Chesworth, K. Kuntz, 2014 .

Discovery of an inhibitor of insulin-like growth factor 1 receptor activation: implications for cellular potency and selectivity over insulin receptor.

E. Alvarez, L. Shewchuk, H. Xie, 2009, Biochemical pharmacology.

Reaction coupling between wild-type and disease-associated mutant EZH2.

Lei Jin, R. Copeland, R. Pollock, 2014, ACS chemical biology.

A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening

K. Swinger, M. Scholle, R. Copeland, 2015, Journal of biomolecular screening.

Mutant Non-Hodgkin Lymphoma EZH 2 Activity in Selective Inhibition of EZH 2 by EPZ-6438 Leads to Potent Antitumor

Yonghong Xiao, R. Copeland, N. Waters, 2014 .

Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation

Jodi Gureasko, W. Janzen, T. Riera, 2018, PloS one.

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

R. Copeland, R. Pollock, B. Littlefield, 2014, PloS one.

Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding.

J. Jackson, T. J. Lansing, R. Mook, 2009, Bioorganic & medicinal chemistry letters.

A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants.

M. Niepel, K. Swinger, K. Kunii, 2021, Cell chemical biology.

Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes

K. Swinger, Claudia Beck, D. Wegener, 2019, SLAS discovery : advancing life sciences R & D.

Identification of a peptide inhibitor for the histone methyltransferase WHSC1

K. Swinger, M. Morrison, W. Janzen, 2018, PloS one.

A Medium-Throughput Single Cell CRISPR-Cas9 Assay to Assess Gene Essentiality

J. Moore, R. Copeland, A. Grassian, 2015, Biological Procedures Online.

Regioselective Synthesis of Benzimidazole Thiophene Inhibitors of Polo‐Like Kinase 1.

M. Cheung, J. Salovich, K. Hornberger, 2009 .

Combinatorial catalyst discovery.

M. Snapper, A. Hoveyda, K. Kuntz, 1999, Current opinion in chemical biology.

Abstract 1344: Small molecule inhibitor of CD38 modulates its intra- and extracellular functions leading to antitumor activity

M. Niepel, K. Kunii, V. Richon, 2021, Experimental and Molecular Therapeutics.

Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.

S. Armstrong, Yonghong Xiao, A. Kung, 2011, Cancer cell.

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

E. Olhava, Lei Jin, R. Copeland, 2012, Nature chemical biology.

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

R. Copeland, R. Pollock, V. Richon, 2013, Proceedings of the National Academy of Sciences.

Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L

Lei Jin, R. Copeland, R. Pollock, 2012, Chemical biology & drug design.

Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma

Yonghong Xiao, R. Copeland, N. Waters, 2014, Molecular Cancer Therapeutics.

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

R. Copeland, R. Pollock, V. Richon, 2016, Journal of medicinal chemistry.