Most cited papers from Epizyme (United States)

Epizyme (United States)

What are the most cited papers from Epizyme (United States)?

The most cited paper from Epizyme (United States) is "Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor" (Scott R. Daigle et al., 2011), with 944 citations. Next come "MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1L" (907) and "The promise and peril of chemical probes" (864).

Published TypeFieldAccessCitations

Showing 50 of 60 papers. Every paper with more than 64 citations is listed.

Most cited papers, sortable by citations and release date
#	Paper
1	Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor Scott R. Daigle et al. · Cancer Cell Open access	Jul 2011	944
2	MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1L Kathrin M. Bernt, Nan Zhu, Amit U. Sinha et al. · Cancer Cell Open access	Jul 2011	907
3	The promise and peril of chemical probes C.H. Arrowsmith et al. · Nature Chemical Biology Open access	21 Jul 2015	864
4	Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2 Sarah K. Knutson, Natalie M. Warholic, Tim J. Wigle et al. · Proceedings of the National Academy of Sciences Open access	25 Apr 2013	803
5	A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells Sarah K. Knutson et al. · Nature Chemical Biology	30 Sep 2012	770
6	The drug–target residence time model: a 10-year retrospective Robert A. Copeland · Nature Reviews Drug Discovery Review	18 Dec 2015	754
7	Potent inhibition of DOT1L as treatment of MLL-fusion leukemia Scott R. Daigle, Edward J. Olhava, Carly A. Therkelsen et al. · Blood Open access	25 Jun 2013	742
8	Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas Christopher J. Sneeringer, Margaret Porter Scott, Kevin W. Kuntz et al. · Proceedings of the National Academy of Sciences Open access	15 Nov 2010	691
9	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 Antoîne Italiano, Jean‐Charles Soria, Maud Toulmonde et al. · The Lancet Oncology	9 Apr 2018	633
10	Tazemetostat for patients with relapsed or refractory follicular lymphoma: an open-label, single-arm, multicentre, phase 2 trial Franck Morschhauser et al. · The Lancet Oncology Open access	6 Oct 2020	605
11	A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models Elayne Chan-Penebre et al. · Nature Chemical Biology	27 Apr 2015	561
12	Chemosensitive Relapse in Small Cell Lung Cancer Proceeds through an EZH2-SLFN11 Axis Eric E. Gardner, Benjamin Hoyin Lok, Valentina E. Schneeberger et al. · Cancer Cell Open access	Feb 2017	547
13	Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2 -Mutant Non-Hodgkin Lymphoma Sarah K. Knutson et al. · Molecular Cancer Therapeutics	22 Feb 2014	531
14	The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia Eytan M. Stein et al. · Blood Open access	3 May 2018	468
15	Protein methyltransferases as a target class for drug discovery Robert A. Copeland, Michael E. Solomon, Victoria M. Richon · Nature Reviews Drug Discovery Review	Sep 2009	466
16	Tazemetostat in advanced epithelioid sarcoma with loss of INI1/SMARCB1: an international, open-label, phase 2 basket study Mrinal M. Gounder et al. · The Lancet Oncology	6 Oct 2020	431
17	Loss of BAP1 function leads to EZH2-dependent transformation Lindsay M. LaFave et al. · Nature Medicine Open access	5 Oct 2015	406
18	Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss Andrew Fedoriw et al. · Cancer Cell Open access	27 Jun 2019	365
19	Nivolumab in children and young adults with relapsed or refractory solid tumours or lymphoma (ADVL1412): a multicentre, open-label, single-arm, phase 1–2 trial Kara Lynn Davis, Elizabeth Fox, Melinda S. Merchant et al. · The Lancet Oncology Open access	17 Mar 2020	344
20	Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing Sarah V. Gerhart, Wendy A. Kellner, Christine Thompson et al. · Scientific Reports Open access	20 Jun 2018	216
21	The dynamics of drug-target interactions: drug-target residence time and its impact on efficacy and safety Robert A. Copeland · Expert Opinion on Drug Discovery	29 Mar 2010	207
22	Conformational Adaptation in Drug–Target Interactions and Residence Time Robert A. Copeland · Future Medicinal Chemistry	Sep 2011	205
23	Chemogenetic Analysis of Human Protein Methyltransferases Victoria M. Richon, Danielle E. Johnston, Christopher J. Sneeringer et al. · Chemical Biology & Drug Design Open access	12 May 2011	190
24	Met Activation in Non-Small Cell Lung Cancer Is Associated with de Novo Resistance to EGFR Inhibitors and the Development of Brain Metastasis Elisa Benedettini, Lynette Marie Sholl, Michael Peyton et al. · American Journal Of Pathology Open access	20 May 2010	186
25	Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l Aniruddha J. Deshpande, Liying Chen, Maurizio Fazio et al. · Blood Open access	30 Jan 2013	177
26	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 Elayne Chan-Penebre, Kelli A. Armstrong, Allison E. Drew et al. · Molecular Cancer Therapeutics Open access	14 Mar 2017	175
27	The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat Kevin W. Kuntz, John E. Campbell, Heike Keilhack et al. · Journal of Medicinal Chemistry Open access	15 Jan 2016	175
28	Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666 Kenneth W. Duncan, Nathalie Rioux, P. Ann Boriack‐Sjodin et al. · ACS Medicinal Chemistry Letters Open access	2 Dec 2015	163
29	Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L Aravind Basavapathruni, Lei Jin, Scott R. Daigle et al. · Chemical Biology & Drug Design Open access	15 Sep 2012	146
30	PRC2 and SWI/SNF Chromatin Remodeling Complexes in Health and Disease Cigall Kadoch, Robert A. Copeland, Heike Keilhack · Biochemistry	2 Feb 2016	144
31	A687V EZH2 is a gain‐of‐function mutation found in lymphoma patients Christina R. Majer, Lei Jin, Margaret Porter Scott et al. · FEBS Letters	28 Jul 2012	143
32	Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma Allison E. Drew et al. · Scientific Reports Open access	15 Dec 2017	142
33	Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound Lorna H. Mitchell, Allison E. Drew, Scott A. Ribich et al. · ACS Medicinal Chemistry Letters Open access	6 Apr 2015	142
34	Therapeutic targeting of cathepsin C: from pathophysiology to treatment Brice Korkmaz, George H. Caughey, Iain Chapple et al. · Pharmacology & Therapeutics Open access	26 May 2018	140
35	EZH2 inhibitor tazemetostat in patients with relapsed or refractory, BAP1-inactivated malignant pleural mesothelioma: a multicentre, open-label, phase 2 study Marjorie Glass Zauderer, Peter Wojciech Szlosarek, Sylvestre Le Moulec et al. · The Lancet Oncology	16 May 2022	138
36	Abrogation of MLL–AF10 and CALM–AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l Liang Chen, Anagha J. Deshpande, Deepti Banka et al. · Leukemia Open access	9 Nov 2012	132
37	EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity John E. Campbell, Kevin W. Kuntz, Sarah K. Knutson et al. · ACS Medicinal Chemistry Letters Open access	4 Mar 2015	131
38	DOT1L as a therapeutic target for the treatment of DNMT3A-mutant acute myeloid leukemia Rachel E. Rau, Blanca Rodríguez, Min Luo et al. · Blood Open access	23 Jun 2016	128
39	DOT1L Inhibitor EPZ-5676 Displays Synergistic Antiproliferative Activity in Combination with Standard of Care Drugs and Hypomethylating Agents in MLL-Rearranged Leukemia Cells Christine R. Klaus, Dorothy Iwanowicz, Danielle E. Johnston et al. · Journal of Pharmacology and Experimental Therapeutics	4 Jul 2014	128
40	Initial testing (stage 1) of tazemetostat (EPZ‐6438), a novel EZH2 inhibitor, by the Pediatric Preclinical Testing Program Raushan T. Kurmasheva, Melissa C. Sammons, Edward Favours et al. · Pediatric Blood & Cancer Open access	24 Aug 2016	124
41	Genetic and evolutionary patterns of treatment resistance in relapsed B-cell lymphoma Christopher K. Rushton et al. · Blood Advances Open access	26 Jun 2020	123
42	Impact of enzyme concentration and residence time on apparent activity recovery in jump dilution analysis Robert A. Copeland, Aravind Basavapathruni, Mikel P. Moyer et al. · Analytical Biochemistry	27 May 2011	113
43	Targeting epigenetic enzymes for drug discovery Robert A. Copeland, Edward J. Olhava, Margaret Porter Scott · Current Opinion in Chemical Biology Review	11 Jul 2010	105
44	The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states Tim J. Wigle, Sarah K. Knutson, Lei Jin et al. · FEBS Letters Open access	17 Aug 2011	91
45	Overcoming Immune Checkpoint Blockade Resistance via EZH2 Inhibition Hye Jung Kim, Harvey Cantor, Kat Cosmopoulos · Trends in Immunology ReviewOpen access	24 Sep 2020	90
46	Final Report of Phase 1 Study of the DOT1L Inhibitor, Pinometostat (EPZ-5676), in Children with Relapsed or Refractory MLL-r Acute Leukemia Neerav Narendra Shukla, Cynthia Wetmore, Maureen Megan O'Brien et al. · Blood	2 Dec 2016	90
47	SWI/SNF component ARID1A restrains pancreatic neoplasia formation Sam C. Wang, Ibrahim Nassour, Shu Xiao et al. · Gut Open access	12 Oct 2018	88
48	Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor Lorna H. Mitchell et al. · ACS Medicinal Chemistry Letters Open access	27 Aug 2015	84
49	Protein Methyltransferases: A Distinct, Diverse, and Dynamic Family of Enzymes P. Ann Boriack‐Sjodin, Kerren K. Swinger · Biochemistry	10 Dec 2015	83
50	Targeting epigenetic regulators for cancer therapy Susan Wee, Dash Dhanak, Haitao Li et al. · Annals of the New York Academy of Sciences	Feb 2014	80

Citations are OpenAlex's own counts, from its 2026-09-23 snapshot, so the ranking can differ from Google Scholar or Web of Science. A paper is listed for an institution when any of its authors gave it as an affiliation; retracted papers and papers whose citation count cannot be traced to citing works are left out, and a preprint and the article it became are shown once. Release dates are OpenAlex's: where a source gave only a month or a year, that is what is shown. How the lists are chosen.