Publications by authors named "Nathalie Rioux"

30Publications

Metabolic disposition of H3B-8800, an orally available small-molecule splicing modulator, in rats, monkeys, and humans.

Authors:
Nathalie Rioux Sherri Smith Federico Colombo Amy Kim W George Lai Darrell Nix Y Amy Siu Joanne Schindler Peter G Smith

Xenobiotica 2020 Sep 6;50(9):1101-1114. Epub 2020 Jan 6.

H3 Biomedicine, Cambridge, MA, USA.

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September 2020

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:

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July 2019

Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERα covalent antagonist (SERCA).

Authors:
Nathalie Rioux Sherri Smith Manav Korpal Morgan O'Shea Sudeep Prajapati Guo Zhu Zheng Markus Warmuth Peter G Smith

Cancer Chemother Pharmacol 2019 01 1;83(1):151-160. Epub 2018 Nov 1.

H3 Biomedicine Inc, 300 Technology Square, Cambridge, MA, 02139, USA.

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January 2019

Effect of a high-fat meal on the relative bioavailability of H3B-6527, a novel FGFR4 inhibitor, in healthy volunteers.

Authors:
Nathalie Rioux Amy Kim Darrell Nix Todd Bowser Markus Warmuth Peter G Smith Joanne Schindler

Cancer Chemother Pharmacol 2019 01 27;83(1):91-96. Epub 2018 Oct 27.

H3 Biomedicine Inc, 300 Technology Square, Cambridge, MA, 02139, USA.

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January 2019

Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERα and ERα Breast Cancer.

Authors:
Xiaoling Puyang Craig Furman Guo Zhu Zheng Zhenhua J Wu Deepti Banka Kiran Aithal Sergei Agoulnik David M Bolduc Silvia Buonamici Benjamin Caleb Subhasree Das Sean Eckley Peter Fekkes Ming-Hong Hao Andrew Hart René Houtman Sean Irwin Jaya J Joshi Craig Karr Amy Kim Namita Kumar Pavan Kumar Galina Kuznetsov Weidong G Lai Nicholas Larsen Crystal Mackenzie Lesley-Ann Martin Diana Melchers Alyssa Moriarty Tuong-Vi Nguyen John Norris Morgan O'Shea Sunil Pancholi Sudeep Prajapati Sujatha Rajagopalan Dominic J Reynolds Victoria Rimkunas Nathalie Rioux Ricardo Ribas Amy Siu Sasirekha Sivakumar Vanitha Subramanian Michael Thomas Frédéric H Vaillancourt John Wang Suzanne Wardell Michael J Wick Shihua Yao Lihua Yu Markus Warmuth Peter G Smith Ping Zhu Manav Korpal

Cancer Discov 2018 09 10;8(9):1176-1193. Epub 2018 Jul 10.

H3 Biomedicine, Inc., Cambridge, Massachusetts.

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September 2018

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

Authors:
Michael J Thomenius Jennifer Totman Darren Harvey Lorna H Mitchell Thomas V Riera Kat Cosmopoulos Alexandra R Grassian Christine Klaus Megan Foley Elizabeth A Admirand Haris Jahic Christina Majer Tim Wigle Suzanne L Jacques Jodi Gureasko Dorothy Brach Trupti Lingaraj Kip West Sherri Smith Nathalie Rioux Nigel J Waters Cuyue Tang Alejandra Raimondi Michael Munchhof James E Mills Scott Ribich Margaret Porter Scott Kevin W Kuntz William P Janzen Mikel Moyer Jesse J Smith Richard Chesworth Robert A Copeland P Ann Boriack-Sjodin

PLoS One 2018 1;13(6):e0197372. Epub 2018 Jun 1.

Epizyme, Inc., Cambridge, Massachusetts, United States of America.

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December 2018

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.

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December 2017

H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma.

Authors:
Jaya Julie Joshi Heather Coffey Erik Corcoran Jennifer Tsai Chia-Ling Huang Kana Ichikawa Sudeep Prajapati Ming-Hong Hao Suzanna Bailey Jeremy Wu Victoria Rimkunas Craig Karr Vanitha Subramanian Pavan Kumar Crystal MacKenzie Raelene Hurley Takashi Satoh Kun Yu Eunice Park Nathalie Rioux Amy Kim Weidong G Lai Lihua Yu Ping Zhu Silvia Buonamici Nicholas Larsen Peter Fekkes John Wang Markus Warmuth Dominic J Reynolds Peter G Smith Anand Selvaraj

Cancer Res 2017 12;77(24):6999-7013

H3 Biomedicine, Cambridge, Massachusetts.

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December 2017

Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.

Authors:
Lee D Fader Murray Bailey Eric Beaulieu François Bilodeau Pierre Bonneau Yves Bousquet Rebekah J Carson Catherine Chabot René Coulombe Jianmin Duan Craig Fenwick Michel Garneau Ted Halmos Araz Jakalian Clint James Stephen H Kawai Serge Landry Steven R LaPlante Stephen W Mason Sebastien Morin Nathalie Rioux Bruno Simoneau Simon Surprenant Bounkham Thavonekham Carl Thibeault Thao Trinh Youla Tsantrizos Jennifer Tsoung Christiane Yoakim Dominik Wernic

ACS Med Chem Lett 2016 Aug 9;7(8):797-801. Epub 2016 Jun 9.

Research and Development, Boehringer Ingelheim (Canada) Ltd. , 2100 Cunard Street, Laval, Québec H7S 2G5, Canada.

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August 2016

CD95-Mediated Calcium Signaling Promotes T Helper 17 Trafficking to Inflamed Organs in Lupus-Prone Mice.

Authors:
Amanda Poissonnier Doriane Sanséau Matthieu Le Gallo Marine Malleter Nicolas Levoin Roselyne Viel Lucie Morere Aubin Penna Patrick Blanco Alain Dupuy Florence Poizeau Alain Fautrel Julien Seneschal Florence Jouan Jerome Ritz Edouard Forcade Nathalie Rioux Cécile Contin-Bordes Thomas Ducret Anne-Marie Vacher Paul A Barrow Robin J Flynn Pierre Vacher Patrick Legembre

Immunity 2016 07;45(1):209-23

Centre Eugène Marquis, Rue Bataille Flandres Dunkerque, 35042 Rennes, France; INSERM ERL440-OSS, Equipe Labellisée, Ligue Contre Le Cancer, 35042 Rennes, France; Université de Rennes 1, 2 Ave. du Prof. Léon Bernard, 35043 Rennes, France; Biosit, Plateforme H2P2, Biogenouest, 2 Ave. du Prof. Léon Bernard, 35043 Rennes, France. Electronic address:

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July 2016

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.

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February 2016

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

Authors:
Lorna H Mitchell P Ann Boriack-Sjodin Sherri Smith Michael Thomenius Nathalie Rioux Michael Munchhof James E Mills Christine Klaus Jennifer Totman Thomas V Riera Alejandra Raimondi Suzanne L Jacques Kip West Megan Foley Nigel J Waters Kevin W Kuntz Tim J Wigle Margaret Porter Scott Robert A Copeland Jesse J Smith Richard Chesworth

ACS Med Chem Lett 2016 Feb 27;7(2):134-8. Epub 2015 Aug 27.

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

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February 2016

Physiologically Based Pharmacokinetic Modeling in Pediatric Oncology Drug Development.

Authors:
Nathalie Rioux Nigel J Waters

Drug Metab Dispos 2016 07 2;44(7):934-43. Epub 2016 Mar 2.

Epizyme Inc., Cambridge, Massachusetts

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July 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

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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.

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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.

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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.

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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.)

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July 2015

Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor.

Authors:
Craig Fenwick Ma'an Amad Murray D Bailey Richard Bethell Michael Bös Pierre Bonneau Michael Cordingley René Coulombe Jianmin Duan Paul Edwards Lee D Fader Anne-Marie Faucher Michel Garneau Araz Jakalian Stephen Kawai Louie Lamorte Steven LaPlante Laibin Luo Steve Mason Marc-André Poupart Nathalie Rioux Patricia Schroeder Bruno Simoneau Sonia Tremblay Youla Tsantrizos Myriam Witvrouw Christiane Yoakim

Antimicrob Agents Chemother 2014 Jun 24;58(6):3233-44. Epub 2014 Mar 24.

Biological Sciences and Chemistry Departments, Boehringer Ingelheim (Canada) Ltd., Research and Development, Laval, QC, Canada.

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June 2014

Assessment of CYP3A-mediated drug-drug interaction potential for victim drugs using an in vivo rat model.

Authors:
Nathalie Rioux Edith Bellavance Serge Bourg Michel Garneau Maria D Ribadeneira Jianmin Duan

Biopharm Drug Dispos 2013 Oct 14;34(7):396-401. Epub 2013 Aug 14.

Biological Sciences, Boehringer-Ingelheim (Canada) Ltd, 2100 Cunard Street, Laval, Québec, Canada, H7S 2G5.

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October 2013