Publications by authors named "Mikel P Moyer"

24Publications

Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss.

Authors:
Andrew Fedoriw Satyajit R Rajapurkar Shane O'Brien Sarah V Gerhart Lorna H Mitchell Nicholas D Adams Nathalie Rioux Trupti Lingaraj Scott A Ribich Melissa B Pappalardi Niyant Shah Jenny Laraio Yan Liu Michael Butticello Chris L Carpenter Caretha Creasy Susan Korenchuk Michael T McCabe Charles F McHugh Raman Nagarajan Craig Wagner Francesca Zappacosta Roland Annan Nestor O Concha Roberta A Thomas Timothy K Hart Jesse J Smith Robert A Copeland Mikel P Moyer John Campbell Kim Stickland James Mills Suzanne Jacques-O'Hagan Christina Allain Danielle Johnston Alejandra Raimondi Margaret Porter Scott Nigel Waters Kerren Swinger Ann Boriack-Sjodin Tom Riera Gideon Shapiro Richard Chesworth Rabinder K Prinjha Ryan G Kruger Olena Barbash Helai P Mohammad

Cancer Cell 2019 07 27;36(1):100-114.e25. Epub 2019 Jun 27.

Epigenetics Research Unit, GlaxoSmithKline, Collegeville, PA 19426, USA. Electronic address:

View Article and Find Full Text PDF
July 2019

Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.

Authors:
Allison E Drew Oscar Moradei Suzanne L Jacques Nathalie Rioux Ann P Boriack-Sjodin Christina Allain Margaret Porter Scott Lei Jin Alejandra Raimondi Jessica L Handler Heidi M Ott Ryan G Kruger Michael T McCabe Christopher Sneeringer Thomas Riera Gideon Shapiro Nigel J Waters Lorna H Mitchell Kenneth W Duncan Mikel P Moyer Robert A Copeland Jesse Smith Richard Chesworth Scott A Ribich

Sci Rep 2017 12 21;7(1):17993. Epub 2017 Dec 21.

Epizyme, Inc., Cambridge, Massachusetts, USA.

View Article and Find Full Text PDF
December 2017

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.

Authors:
Kenneth W Duncan Nathalie Rioux P Ann Boriack-Sjodin Michael J Munchhof Lawrence A Reiter Christina R Majer Lei Jin L Danielle Johnston Elayne Chan-Penebre Kristy G Kuplast Margaret Porter Scott Roy M Pollock Nigel J Waters Jesse J Smith Mikel P Moyer Robert A Copeland Richard Chesworth

ACS Med Chem Lett 2016 Feb 2;7(2):162-6. Epub 2015 Dec 2.

Epizyme, Inc. , 400 Technology Square, Cambridge, Massachusetts 02139, United States.

View Article and Find Full Text PDF
February 2016

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

Authors:
Kevin W Kuntz John E Campbell Heike Keilhack Roy M Pollock Sarah K Knutson Margaret Porter-Scott Victoria M Richon Chris J Sneeringer Tim J Wigle Christina J Allain Christina R Majer Mikel P Moyer Robert A Copeland Richard Chesworth

J Med Chem 2016 Feb 27;59(4):1556-64. Epub 2016 Jan 27.

Epizyme , 400 Technology Square, Fourth Floor, Cambridge, Massachusetts 02139, United States.

View Article and Find Full Text PDF
February 2016

Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human.

Authors:
Nigel J Waters Sherri A Smith Edward J Olhava Kenneth W Duncan Richard D Burton James O'Neill Marie-Eve Rodrigue Roy M Pollock Mikel P Moyer Richard Chesworth

Cancer Chemother Pharmacol 2016 Jan 8;77(1):43-62. Epub 2015 Dec 8.

Epizyme, Inc., 400 Technology Square, Cambridge, MA, 02139, USA.

View Article and Find Full Text PDF
January 2016

Structural Insights into Ternary Complex Formation of Human CARM1 with Various Substrates.

Authors:
P Ann Boriack-Sjodin Lei Jin Suzanne L Jacques Allison Drew Chris Sneeringer Margaret Porter Scott Mikel P Moyer Scott Ribich Oscar Moradei Robert A Copeland

ACS Chem Biol 2016 Mar 23;11(3):763-71. Epub 2015 Nov 23.

Epizyme, Inc. 400 Technology Square, Cambridge, Massachusetts 02139, United States.

View Article and Find Full Text PDF
March 2016

Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor.

Authors:
Nathalie Rioux Kenneth W Duncan Ronald J Lantz Xiusheng Miao Elayne Chan-Penebre Mikel P Moyer Michael J Munchhof Robert A Copeland Richard Chesworth Nigel J Waters

Xenobiotica 2016 ;46(3):268-77

View Article and Find Full Text PDF
October 2016

Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.

Authors:
Lorna H Mitchell Allison E Drew Scott A Ribich Nathalie Rioux Kerren K Swinger Suzanne L Jacques Trupti Lingaraj P Ann Boriack-Sjodin Nigel J Waters Tim J Wigle Oscar Moradei Lei Jin Tom Riera Margaret Porter-Scott Mikel P Moyer Jesse J Smith Richard Chesworth Robert A Copeland

ACS Med Chem Lett 2015 Jun 6;6(6):655-9. Epub 2015 Apr 6.

Epizyme, Inc. , 400 Technology Square, Fourth Floor, Cambridge, Massachusetts 02138, United States.

View Article and Find Full Text PDF
June 2015

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

Authors:
John E Campbell Kevin W Kuntz Sarah K Knutson Natalie M Warholic Heike Keilhack Tim J Wigle Alejandra Raimondi Christine R Klaus Nathalie Rioux Akira Yokoi Satoshi Kawano Yukinori Minoshima Hyeong-Wook Choi Margaret Porter Scott Nigel J Waters Jesse J Smith Richard Chesworth Mikel P Moyer Robert A Copeland

ACS Med Chem Lett 2015 May 4;6(5):491-5. Epub 2015 Mar 4.

Epizyme, Inc. , 400 Technology Square, Fourth Floor, Cambridge, Massachusetts 02139, United States.

View Article and Find Full Text PDF
May 2015

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.

Authors:
Elayne Chan-Penebre Kristy G Kuplast Christina R Majer P Ann Boriack-Sjodin Tim J Wigle L Danielle Johnston Nathalie Rioux Michael J Munchhof Lei Jin Suzanne L Jacques Kip A West Trupti Lingaraj Kimberly Stickland Scott A Ribich Alejandra Raimondi Margaret Porter Scott Nigel J Waters Roy M Pollock Jesse J Smith Olena Barbash Melissa Pappalardi Thau F Ho Kelvin Nurse Khyati P Oza Kathleen T Gallagher Ryan Kruger Mikel P Moyer Robert A Copeland Richard Chesworth Kenneth W Duncan

Nat Chem Biol 2015 Jun 27;11(6):432-7. Epub 2015 Apr 27.

Departments of Biology and Molecular Discovery, Epizyme, Inc., Cambridge, Massachusetts, USA.

View Article and Find Full Text PDF
June 2015

Structural and Kinetic Characterization of a Novel N-acetylated Aliphatic Amine Metabolite of the PRMT Inhibitor, EPZ011652.

Authors:
Nathalie Rioux Lorna H Mitchell Philip Tiller Katie Plant Joanne Shaw Kerry Frost Scott Ribich Mikel P Moyer Robert A Copeland Richard Chesworth Nigel J Waters

Drug Metab Dispos 2015 Jul 17;43(7):936-43. Epub 2015 Apr 17.

Epizyme, Cambridge, Massachusetts (N.R., L.H.M., S.R., M.P.M., R.A.C., R.C., N.J.W.); RMI Laboratories, North Wales, Pennsylvania (P.T.); and Cyprotex, Macclesfield, Cheshire, United Kingdom (K.P., J.S., K.F.)

View Article and Find Full Text PDF
July 2015

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

Authors:
Tim J Wigle Kerren K Swinger John E Campbell Michael D Scholle John Sherrill Elizabeth A Admirand P Ann Boriack-Sjodin Kevin W Kuntz Richard Chesworth Mikel P Moyer Margaret Porter Scott Robert A Copeland

J Biomol Screen 2015 Jul 9;20(6):810-20. Epub 2015 Mar 9.

Epizyme, Inc., Cambridge, MA, USA.

View Article and Find Full Text PDF
July 2015

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

Authors:
Sarah K Knutson Natalie M Warholic L Danielle Johnston Christine R Klaus Tim J Wigle Dorothy Iwanowicz Bruce A Littlefield Margaret Porter-Scott Jesse J Smith Mikel P Moyer Robert A Copeland Roy M Pollock Kevin W Kuntz Alejandra Raimondi Heike Keilhack

PLoS One 2014 10;9(12):e111840. Epub 2014 Dec 10.

Research and Development, Epizyme Inc., Cambridge, Massachusetts, United States of America.

View Article and Find Full Text PDF
October 2017

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

Authors:
Brooke M Swalm Sarah K Knutson Natalie M Warholic Lei Jin Kevin W Kuntz Heike Keilhack Jesse J Smith Roy M Pollock Mikel P Moyer Margaret Porter Scott Robert A Copeland Tim J Wigle

ACS Chem Biol 2014 Nov 28;9(11):2459-64. Epub 2014 Aug 28.

Epizyme, Inc. 400 Technology Square, Fourth Floor, Cambridge, Massachusetts 02139, United States.

View Article and Find Full Text PDF
November 2014

DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells.

Authors:
Christine R Klaus Dorothy Iwanowicz Danielle Johnston Carly A Campbell Jesse J Smith Mikel P Moyer Robert A Copeland Edward J Olhava Margaret Porter Scott Roy M Pollock Scott R Daigle Alejandra Raimondi

J Pharmacol Exp Ther 2014 Sep 3;350(3):646-56. Epub 2014 Jul 3.

Epizyme Inc., Cambridge, Massachusetts

View Article and Find Full Text PDF
September 2014

Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.

Authors:
Sarah K Knutson Satoshi Kawano Yukinori Minoshima Natalie M Warholic Kuan-Chun Huang Yonghong Xiao Tadashi Kadowaki Mai Uesugi Galina Kuznetsov Namita Kumar Tim J Wigle Christine R Klaus Christina J Allain Alejandra Raimondi Nigel J Waters Jesse J Smith Margaret Porter-Scott Richard Chesworth Mikel P Moyer Robert A Copeland Victoria M Richon Toshimitsu Uenaka Roy M Pollock Kevin W Kuntz Akira Yokoi Heike Keilhack

Mol Cancer Ther 2014 Apr 21;13(4):842-54. Epub 2014 Feb 21.

Authors' Affiliations: Epizyme Inc., Cambridge; Eisai Inc., Andover, Massachusetts; and Eisai Co. Ltd., Tsukuba-shi, Ibaraki, Japan.

View Article and Find Full Text PDF
April 2014

Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.

Authors:
Aravind Basavapathruni Edward J Olhava Scott R Daigle Carly A Therkelsen Lei Jin P Ann Boriack-Sjodin Christina J Allain Christine R Klaus Alejandra Raimondi Margaret Porter Scott Angelos Dovletoglou Victoria M Richon Roy M Pollock Robert A Copeland Mikel P Moyer Richard Chesworth Paul G Pearson Nigel J Waters

Biopharm Drug Dispos 2014 May 14;35(4):237-52. Epub 2014 Feb 14.

Epizyme Inc., 400 Technology Square, Cambridge, MA, USA.

View Article and Find Full Text PDF
May 2014

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia.

Authors:
Scott R Daigle Edward J Olhava Carly A Therkelsen Aravind Basavapathruni Lei Jin P Ann Boriack-Sjodin Christina J Allain Christine R Klaus Alejandra Raimondi Margaret Porter Scott Nigel J Waters Richard Chesworth Mikel P Moyer Robert A Copeland Victoria M Richon Roy M Pollock

Blood 2013 Aug 25;122(6):1017-25. Epub 2013 Jun 25.

Epizyme, Inc., 400 Technology Square, Cambridge, MA 02139, USA.

View Article and Find Full Text PDF
August 2013

Convergent evolution of chromatin modification by structurally distinct enzymes: comparative enzymology of histone H3 Lys²⁷ methylation by human polycomb repressive complex 2 and vSET.

Authors:
Brooke M Swalm Kenneth K Hallenbeck Christina R Majer Lei Jin Margaret Porter Scott Mikel P Moyer Robert A Copeland Tim J Wigle

Biochem J 2013 Jul;453(2):241-7

Epizyme Inc., 400 Technology Square, Cambridge, MA 02139, USA.

View Article and Find Full Text PDF
July 2013

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

Authors:
Sarah K Knutson Natalie M Warholic Tim J Wigle Christine R Klaus Christina J Allain Alejandra Raimondi Margaret Porter Scott Richard Chesworth Mikel P Moyer Robert A Copeland Victoria M Richon Roy M Pollock Kevin W Kuntz Heike Keilhack

Proc Natl Acad Sci U S A 2013 May 25;110(19):7922-7. Epub 2013 Apr 25.

Epizyme, Inc, Cambridge, MA 02139, USA.

View Article and Find Full Text PDF
May 2013