H. Keilhack

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.

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

Yonghong Xiao, R. Copeland, A. Grassian, 2016, PloS one.

Regulation of Brown Fat Adipogenesis by Protein Tyrosine Phosphatase 1B

F. Haj, H. Keilhack, N. Nagata, 2011, PloS one.

Small molecule inhibitors of EZH2: the emerging translational landscape.

H. Keilhack, Jesse J. Smith, 2015, Epigenomics.

The Protein-tyrosine Phosphatase SHP-1 Binds to and Dephosphorylates p120 Catenin*

U. Hellman, F. van Roy, J. Godovac-Zimmermann, 2000, The Journal of Biological Chemistry.

Selective pharmaceutical inhibition of PARP14 mitigates allergen-induced IgE and mucus overproduction in a mouse model of pulmonary allergic response

Kevin C. Chen, M. Niepel, K. Swinger, 2021, bioRxiv.

EZH2 Modifies Sunitinib Resistance in Renal Cell Carcinoma by Kinome Reprogramming.

Peter C. Hollenhorst, M. Seshadri, W. Tao, 2017, Cancer research.

302 A phase 1 study of EPZ-6438 (E7438), an Enhancer of Zeste-Homolog 2 (EZH2) inhibitor: Preliminary activity in INI1-negative tumors

J. Coindre, M. Toulmonde, A. Italiano, 2015 .

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

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

Binding of phosphatidic acid to the protein-tyrosine phosphatase SHP-1 as a basis for activity modulation.

O. Zschörnig, F. Böhmer, H. Keilhack, 1999, Biochemistry.

Reply to "Uveal melanoma cells are resistant to EZH2 inhibition regardless of BAP1 status"

S. Armstrong, N. Kelleher, E. Stanchina, 2016, Nature Medicine.

Loss of BAP1 function leads to EZH2-dependent transformation

S. Armstrong, N. Kelleher, O. Abdel-Wahab, 2015, Nature Medicine.

Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule

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

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

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

In Vitro Long-Term Proliferation Assays to Study Antiproliferative Effects of PARP Inhibitors on Cancer Cells.

P. Chang, H. Keilhack, 2017, Methods in molecular 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 .

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.

6LBA Phase 1 first-in-human study of the enhancer of zeste-homolog 2 (EZH2) histone methyl transferase inhibitor E7438 as a single agent in patients with advanced solid tumors or B cell lymphoma

A. Italiano, J. Soria, R. Chen, 2014 .

Final results of a translational phase l study assessing a QOD schedule of the potent AKT inhibitor MK-2206 incorporating predictive, pharmacodynamic (PD), and functional imaging biomarkers.

A. Tolcher, N. Tunariu, A. Patnaik, 2011, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

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.

Identification of Src Phosphorylation Sites in the Catenin p120 ctn *

A. Reynolds, P. Anastasiadis, F. Böhmer, 2001, The Journal of Biological Chemistry.

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.

Prognostic, therapeutic, and mechanistic implications of a mouse model of leukemia evoked by Shp2 (PTPN11) mutations.

J. Kutok, K. Akashi, B. Neel, 2005, Cancer cell.

PDK1 attenuation fails to prevent tumor formation in PTEN-deficient transgenic mouse models.

K. Kunii, R. Bronson, M. Scott, 2011, Cancer research.

Therapeutics , Targets , and Chemical Biology PDK 1 Attenuation Fails to Prevent Tumor Formation in PTEN-Deficient Transgenic Mouse Models

Hare, K. Kunii, R. Bronson, 2011 .

Genetic and Pharmacological Inhibition of PDK1 in Cancer Cells

C. Paweletz, Youwei Yan, M. Wiznerowicz, 2010, The Journal of Biological Chemistry.

Sensitive multiplexed analysis of kinase activities and activity-based kinase identification

S. Gygi, C. Paweletz, J. Villén, 2009, Nature Biotechnology.

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

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

Diverse Biochemical Properties of Shp2 Mutants

Malcolm McGregor, Lewis C Cantley, M. McGregor, 2005, Journal of Biological Chemistry.

Activating Mutations of the Noonan Syndrome-Associated SHP2/PTPN11 Gene in Human Solid Tumors and Adult Acute Myelogenous Leukemia

John D. Minna, John M. Maris, Victor E. Velculescu, 2004, Cancer Research.

Advances in Brief Activating Mutations of the Noonan Syndrome-Associated SHP 2 / PTPN 11 Gene in Human Solid Tumors and Adult Acute Myelogenous Leukemia

M. Loh, M. Meyerson, W. Sellers, 2004 .

Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study.

T. Owa, C. Lucchesi, J. Coindre, 2018, The Lancet. Oncology.

Initial testing (stage 1) of tazemetostat (EPZ‐6438), a novel EZH2 inhibitor, by the Pediatric Preclinical Testing Program

P. Houghton, Katherine Cosmopoulos, Malcolm A. Smith, 2017, Pediatric blood & cancer.

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

R. Copeland, Cigall Kadoch, H. Keilhack, 2016, Biochemistry.

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

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

Comparative expression analysis of four breast cancer subtypes versus matched normal tissue from the same patients

Deanne M. Taylor, J. Bienkowska, P. Martini, 2008, The Journal of Steroid Biochemistry and Molecular Biology.

Negative Regulation of Ros Receptor Tyrosine Kinase Signaling

W. Birchmeier, C. Birchmeier, H. Kosmehl, 2001, The Journal of cell biology.

Both SH2 Domains Are Involved in Interaction of SHP-1 with the Epidermal Growth Factor Receptor but Cannot Confer Receptor-directed Activity to SHP-1/SHP-2 Chimera*

A. Ullrich, S. Tomić, T. Tenev, 1997, The Journal of Biological Chemistry.

Evidence of mTOR Activation by an AKT-Independent Mechanism Provides Support for the Combined Treatment of PTEN-Deficient Prostate Tumors with mTOR and AKT Inhibitors.

C. Paweletz, P. Majumder, K. Kunii, 2012, Translational oncology.

Differential Regulation of Endoplasmic Reticulum Stress by Protein Tyrosine Phosphatase 1B and T Cell Protein Tyrosine Phosphatase*

F. Haj, Siming Liu, T. Tiganis, 2011, The Journal of Biological Chemistry.

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 .

Phase 1 Study of Tazemetostat (EPZ-6438), an Inhibitor of Enhancer of Zeste-Homolog 2 (EZH2): Preliminary Safety and Activity in Relapsed or Refractory Non-Hodgkin Lymphoma (NHL) Patients

A. Italiano, J. Soria, A. Mcdonald, 2015 .

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

I. Feldman, R. Copeland, A. Grassian, 2017, Molecular Cancer Therapeutics.

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.

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.

Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation.

M. Niepel, B. Gui, R. Abo, 2019, Biochemical pharmacology.

Phosphotyrosine 1173 Mediates Binding of the Protein-tyrosine Phosphatase SHP-1 to the Epidermal Growth Factor Receptor and Attenuation of Receptor Signaling*

J Godovac-Zimmermann, T. Tenev, J. Godovac-Zimmermann, 1998, The Journal of Biological Chemistry.

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

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

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

I. Feldman, R. Copeland, A. Raimondi, 2017, Molecular Cancer Therapeutics.

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.

866 RBN-2397, a novel, potent, and selective PARP7 inhibitor, induces tumor-intrinsic type I interferon responses and adaptive immunity in preclinical models and patient tumors

T. Yap, R. Abo, G. Falchook, 2021, Journal for ImmunoTherapy of Cancer.