Thomas H Marsilje

Thomas H Marsilje

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Thomas H Marsilje

Thomas H Marsilje

Publications by authors named "Thomas H Marsilje"

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A Blueprint to Advance Colorectal Cancer Immunotherapies.

Authors:
Dung T Le Vanessa M Hubbard-Lucey Michael A Morse Christopher R Heery Andrea Dwyer Thomas H Marsilje Arthur N Brodsky Emily Chan Dustin A Deming Luis A Diaz Wolf H Fridman Richard M Goldberg Stanley R Hamilton Franck Housseau Elizabeth M Jaffee S Peter Kang Smitha S Krishnamurthi Christopher H Lieu Wells Messersmith Cynthia L Sears Neil H Segal Arvin Yang Rebecca A Moss Edward Cha Jill O'Donnell-Tormey Nancy Roach Anjelica Q Davis Keavy McAbee Sharyn Worrall Al B Benson

Cancer Immunol Res 2017 11 16;5(11):942-949. Epub 2017 Oct 16.

Northwestern University, Chicago, Illinois.

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http://cancerimmunolres.aacrjournals.org/lookup/doi/10.1158/
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http://dx.doi.org/10.1158/2326-6066.CIR-17-0375DOI Listing
November 2017

Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.

Authors:
Gérald Lelais Robert Epple Thomas H Marsilje Yun O Long Matthew McNeill Bei Chen Wenshuo Lu Jaganmohan Anumolu Sangamesh Badiger Badry Bursulaya Michael DiDonato Rina Fong Jose Juarez Jie Li Mari Manuia Daniel E Mason Perry Gordon Todd Groessl Kevin Johnson Yong Jia Shailaja Kasibhatla Chun Li John Isbell Glen Spraggon Steven Bender Pierre-Yves Michellys

J Med Chem 2016 07 19;59(14):6671-89. Epub 2016 Jul 19.

Genomics Institute of the Novartis Research Foundation , 10675 John J. Hopkins Drive, San Diego, California 92121, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.5b01985DOI Listing
July 2016

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.

Authors:
Yong Jia Cai-Hong Yun Eunyoung Park Dalia Ercan Mari Manuia Jose Juarez Chunxiao Xu Kevin Rhee Ting Chen Haikuo Zhang Sangeetha Palakurthi Jaebong Jang Gerald Lelais Michael DiDonato Badry Bursulaya Pierre-Yves Michellys Robert Epple Thomas H Marsilje Matthew McNeill Wenshuo Lu Jennifer Harris Steven Bender Kwok-Kin Wong Pasi A Jänne Michael J Eck

Nature 2016 06 25;534(7605):129-32. Epub 2016 May 25.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, USA.

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http://dx.doi.org/10.1038/nature17960DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4929832PMC
June 2016

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Authors:
Robin A Fairhurst Thomas H Marsilje Stefan Stutz Andreas Boos Michel Niklaus Bei Chen Songchun Jiang Wenshuo Lu Pascal Furet Clive McCarthy Frédéric Stauffer Vito Guagnano Andrea Vaupel Pierre-Yves Michellys Christian Schnell Sébastien Jeay

Bioorg Med Chem Lett 2016 Apr 26;26(8):2057-64. Epub 2016 Feb 26.

Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.

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http://dx.doi.org/10.1016/j.bmcl.2016.02.075DOI Listing
April 2016

EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.

Authors:
Yong Jia Jose Juarez Jie Li Mari Manuia Matthew J Niederst Celin Tompkins Noelito Timple Mei-Ting Vaillancourt AnneMarie Culazzo Pferdekamper Elizabeth L Lockerman Chun Li Jennifer Anderson Carlotta Costa Debbie Liao Eric Murphy Michael DiDonato Badry Bursulaya Gerald Lelais Jordi Barretina Matthew McNeill Robert Epple Thomas H Marsilje Nuzhat Pathan Jeffrey A Engelman Pierre-Yves Michellys Peter McNamara Jennifer Harris Steven Bender Shailaja Kasibhatla

Cancer Res 2016 Mar 29;76(6):1591-602. Epub 2016 Jan 29.

Genomics Institute of the Novartis Research Foundation, San Diego, California.

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http://cancerres.aacrjournals.org/content/early/2016/01/29/0
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http://cancerres.aacrjournals.org/content/76/6/1591.full.pdf
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http://cancerres.aacrjournals.org/cgi/doi/10.1158/0008-5472.
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http://dx.doi.org/10.1158/0008-5472.CAN-15-2581DOI Listing
March 2016

Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.

Authors:
Pierre-Yves Michellys Bei Chen Tao Jiang Yunho Jin Wenshuo Lu Thomas H Marsilje Wei Pei Tetsuo Uno Xuefeng Zhu Baogen Wu Truc Ngoc Nguyen Badry Bursulaya Christian Lee Nanxin Li Sungjoon Kim Tove Tuntland Bo Liu Frank Sun Auzon Steffy Tami Hood

Bioorg Med Chem Lett 2016 Feb 17;26(3):1090-1096. Epub 2015 Nov 17.

Novartis Institutes for BioMedical Research, Inc., 250 Massachusetts Avenue, Cambridge, MA 02139, United States.

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http://dx.doi.org/10.1016/j.bmcl.2015.11.049DOI Listing
February 2016

Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor.

Authors:
Francois Gessier Inga Preuss Hong Yin Mette M Rosenkilde Stephane Laurent Ralf Endres Yu A Chen Thomas H Marsilje Klaus Seuwen Deborah G Nguyen Andreas W Sailer

J Med Chem 2014 Apr 15;57(8):3358-68. Epub 2014 Apr 15.

Global Discovery Chemistry; ‡Developmental & Molecular Pathways, §Analytical Sciences, Novartis Institutes for BioMedical Research , Basel 4002, Switzerland.

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http://pubs.acs.org/doi/10.1021/jm4019355
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http://dx.doi.org/10.1021/jm4019355DOI Listing
April 2014

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.

Authors:
Thomas H Marsilje Wei Pei Bei Chen Wenshuo Lu Tetsuo Uno Yunho Jin Tao Jiang Sungjoon Kim Nanxin Li Markus Warmuth Yelena Sarkisova Frank Sun Auzon Steffy AnneMarie C Pferdekamper Allen G Li Sean B Joseph Young Kim Bo Liu Tove Tuntland Xiaoming Cui Nathanael S Gray Ruo Steensma Yongqin Wan Jiqing Jiang Greg Chopiuk Jie Li W Perry Gordon Wendy Richmond Kevin Johnson Jonathan Chang Todd Groessl You-Qun He Andrew Phimister Alex Aycinena Christian C Lee Badry Bursulaya Donald S Karanewsky H Martin Seidel Jennifer L Harris Pierre-Yves Michellys

J Med Chem 2013 Jul 26;56(14):5675-90. Epub 2013 Jun 26.

Genomics Institute of the Novartis Research Foundation , 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

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http://dx.doi.org/10.1021/jm400402qDOI Listing
July 2013

High-content micronucleus assay in genotoxicity profiling: initial-stage development and some applications in the investigative/lead-finding studies in drug discovery.

Authors:
Madhu S Mondal Joseph Gabriels Claudia McGinnis Maria Magnifico Thomas H Marsilje Laszlo Urban Alan Collis Dejan Bojanic Scott A Biller Wilfried Frieauff Hans-Joerg Martus Willi Suter Philip Bentley

Toxicol Sci 2010 Nov 14;118(1):71-85. Epub 2010 Jul 14.

Preclinical Safety Profiling, CPC, Novartis Institutes of Biomedical Research, Inc., Cambridge, Massachusetts 02139, USA.

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http://dx.doi.org/10.1093/toxsci/kfq181DOI Listing
November 2010

Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.

Authors:
Phil B Alper Thomas H Marsilje Daniel Mutnick Wenshuo Lu Arnab Chatterjee Michael J Roberts Yun He Donald S Karanewsky Donald Chow Jianmin Lao Andrea Gerken Tove Tuntland Bo Liu Jonathan Chang Perry Gordon H Martin Seidel Shin-Shay Tian

Bioorg Med Chem Lett 2008 Oct 22;18(19):5255-8. Epub 2008 Aug 22.

Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.

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http://dx.doi.org/10.1016/j.bmcl.2008.08.068DOI Listing
October 2008

Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold.

Authors:
Thomas H Marsilje Phil B Alper Wenshuo Lu Daniel Mutnick Pierre-Yves Michellys Yun He Donald S Karanewsky Donald Chow Andrea Gerken Jianmin Lao Min-Ju Kim H Martin Seidel Shin-Shay Tian

Bioorg Med Chem Lett 2008 Oct 26;18(19):5259-62. Epub 2008 Aug 26.

Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.

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http://dx.doi.org/10.1016/j.bmcl.2008.08.077DOI Listing
October 2008

NMR structural studies of interactions of a small, nonpeptidyl Tpo mimic with the thrombopoietin receptor extracellular juxtamembrane and transmembrane domains.

Authors:
Min-Ju Kim Sang Ho Park Stanley J Opella Thomas H Marsilje Pierre-Yves Michellys H Martin Seidel Shin-Shay Tian

J Biol Chem 2007 May 16;282(19):14253-61. Epub 2007 Mar 16.

Genomics Institute of the Novartis Research Foundation, San Diego, CA 92121, USA.

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http://dx.doi.org/10.1074/jbc.M611616200DOI Listing
May 2007

Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.

Authors:
Anil Vasudevan Matthew J LaMarche Christopher Blackburn Jennifer Lee Che Courtney A Luchaco-Cullis Sujen Lai Thomas H Marsilje Michael A Patane Andrew J Souers Derek Wodka Bradley Geddes Sumiao Chen Seven Brodjian Doug H Falls Brian D Dayton Eugene Bush Michael Brune Robin D Shapiro Kennan C Marsh Lisa E Hernandez Hing L Sham Christine A Collins Philip R Kym

Bioorg Med Chem Lett 2005 Oct;15(19):4174-9

Metabolic Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA.

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http://dx.doi.org/10.1016/j.bmcl.2005.06.089DOI Listing
October 2005

Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).

Authors:
Thomas H Marsilje Jonathan B Roses Emily F Calderwood Stephen G Stroud Nancy E Forsyth Christopher Blackburn David L Yowe Wenyan Miao Stacey V Drabic Marie D Bohane J Scott Daniels Ping Li Lijun Wu Michael A Patane Christopher F Claiborne

Bioorg Med Chem Lett 2004 Jul;14(14):3721-5

Department of Medicinal Chemistry, Millennium Pharmaceuticals, Inc., Cambridge, MA 02139, USA.

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http://dx.doi.org/10.1016/j.bmcl.2004.05.003DOI Listing
July 2004

Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.

Authors:
Thomas H Marsilje Michael P Hedrick Joel Desharnais Ali Tavassoli Yan Zhang Ian A Wilson Stephen J Benkovic Dale L Boger

Bioorg Med Chem 2003 Oct;11(20):4487-501

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

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http://dx.doi.org/10.1016/s0968-0896(03)00456-5DOI Listing
October 2003

10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase.

Authors:
Thomas H Marsilje Michael P Hedrick Joel Desharnais Kevin Capps Ali Tavassoli Yan Zhang Ian A Wilson Stephen J Benkovic Dale L Boger

Bioorg Med Chem 2003 Oct;11(20):4503-9

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

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http://dx.doi.org/10.1016/s0968-0896(03)00457-7DOI Listing
October 2003

Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid.

Authors:
Yan Zhang Joel Desharnais Thomas H Marsilje Chenglong Li Michael P Hedrick Lata T Gooljarsingh Ali Tavassoli Stephen J Benkovic Arthur J Olson Dale L Boger Ian A Wilson

Biochemistry 2003 May;42(20):6043-56

Department of Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.

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http://dx.doi.org/10.1021/bi034219cDOI Listing
May 2003

10-Formyl-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid (10-formyl-DDACTHF): a potent cytotoxic agent acting by selective inhibition of human GAR Tfase and the de novo purine biosynthetic pathway.

Authors:
Thomas H Marsilje Marc A Labroli Michael P Hedrick Qing Jin Joel Desharnais Stephen J Baker Lata T Gooljarsingh Joseph Ramcharan Ali Tavassoli Yan Zhang Ian A Wilson G Peter Beardsley Stephen J Benkovic Dale L Boger

Bioorg Med Chem 2002 Aug;10(8):2739-49

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

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http://dx.doi.org/10.1016/s0968-0896(02)00102-5DOI Listing
August 2002