Publications by authors named "Markus Wartmann"

44Publications

Discovery of Potent, Highly Selective, and Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing.

Authors:
Carole Pissot Soldermann Oliver Simic Martin Renatus Paulus Erbel Samu Melkko Markus Wartmann Marc Bigaud Andreas Weiss Paul McSheehy Ralf Endres Paulo Santos Jutta Blank Ansgar Schuffenhauer Guido Bold Nicole Buschmann Thomas Zoller Eva Altmann Paul W Manley Ina Dix Elisabeth Buchdunger Julien Scesa Jean Quancard Achim Schlapbach Frédéric Bornancin Thomas Radimerski Catherine H Régnier

J Med Chem 2020 12 30;63(23):14576-14593. Epub 2020 Nov 30.

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

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December 2020

Optimization of the Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood.

Authors:
Jean Quancard Oliver Simic Carole Pissot Soldermann Reiner Aichholz Markus Blatter Martin Renatus Paulus Erbel Samu Melkko Ralf Endres Mickael Sorge Laurence Kieffer Trixie Wagner Karen Beltz Paul Mcsheehy Markus Wartmann Catherine H Régnier Thomas Calzascia Thomas Radimerski Marc Bigaud Andreas Weiss Frédéric Bornancin Achim Schlapbach

J Med Chem 2020 12 20;63(23):14594-14608. Epub 2020 Nov 20.

Novartis Pharma AG, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.

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December 2020

Correction to "2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4".

Authors:
Thomas Knoepfel Pascal Furet Robert Mah Nicole Buschmann Catherine Leblanc Sebastien Ripoche Diana Graus-Porta Markus Wartmann Inga Galuba Robin A Fairhurst

ACS Med Chem Lett 2020 Nov 14;11(11):2341. Epub 2020 Oct 14.

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November 2020

Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.

Authors:
Robin A Fairhurst Thomas Knoepfel Nicole Buschmann Catherine Leblanc Robert Mah Milen Todorov Pierre Nimsgern Sebastien Ripoche Michel Niklaus Nicolas Warin Van Huy Luu Mario Madoerin Jasmin Wirth Diana Graus-Porta Andreas Weiss Michael Kiffe Markus Wartmann Jacqueline Kinyamu-Akunda Dario Sterker Christelle Stamm Flavia Adler Alexandra Buhles Heiko Schadt Philippe Couttet Jutta Blank Inga Galuba Jörg Trappe Johannes Voshol Nils Ostermann Chao Zou Jörg Berghausen Alberto Del Rio Espinola Wolfgang Jahnke Pascal Furet

J Med Chem 2020 11 1;63(21):12542-12573. Epub 2020 Oct 1.

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

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November 2020

FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer.

Authors:
Andreas Weiss Flavia Adler Alexandra Buhles Christelle Stamm Robin A Fairhurst Michael Kiffe Dario Sterker Mario Centeleghe Markus Wartmann Jacqueline Kinyamu-Akunda Heiko S Schadt Philippe Couttet Armin Wolf Youzhen Wang Patrizia Barzaghi-Rinaudo Masato Murakami Audrey Kauffmann Thomas Knoepfel Nicole Buschmann Catherine Leblanc Robert Mah Pascal Furet Jutta Blank Francesco Hofmann William R Sellers Diana Graus Porta

Mol Cancer Ther 2019 12 13;18(12):2194-2206. Epub 2019 Aug 13.

Novartis Institutes for Biomedical Research, Oncology Disease Area, Basel, Switzerland.

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December 2019

Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its Predominant Metabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy.

Authors:
Paul W Manley Giorgio Caravatti Pascal Furet Johannes Roesel Phi Tran Trixie Wagner Markus Wartmann

Biochemistry 2018 09 13;57(38):5576-5590. Epub 2018 Sep 13.

Oncology Disease Area, Novartis Institutes for Biomedical Research , Novartis International AG , CH-4002 Basel , Switzerland.

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September 2018

Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201.

Authors:
Sébastien Jeay Stéphane Ferretti Philipp Holzer Jeanette Fuchs Emilie A Chapeau Markus Wartmann Dario Sterker Vincent Romanet Masato Murakami Grainne Kerr Eric Y Durand Swann Gaulis Marta Cortes-Cros Stephan Ruetz Therese-Marie Stachyra Joerg Kallen Pascal Furet Jens Würthner Nelson Guerreiro Ensar Halilovic Astrid Jullion Audrey Kauffmann Emil Kuriakose Marion Wiesmann Michael R Jensen Francesco Hofmann William R Sellers

Cancer Res 2018 11 22;78(21):6257-6267. Epub 2018 Aug 22.

Disease Area Oncology, Novartis Institutes for BioMedical Research, Cambridge, Massachusetts.

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November 2018

N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity.

Authors:
Achim Schlapbach Laszlo Revesz Carole Pissot Soldermann Thomas Zoller Catherine H Régnier Frédéric Bornancin Thomas Radimerski Jutta Blank Ansgar Schuffenhauer Martin Renatus Paulus Erbel Samu Melkko Richard Heng Oliver Simic Ralf Endres Markus Wartmann Jean Quancard

Bioorg Med Chem Lett 2018 07 9;28(12):2153-2158. Epub 2018 May 9.

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

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July 2018

Continuous low-dose infusion of patupilone increases the therapeutic index in mouse and rat tumour models.

Authors:
Mike Becquet Laurent Laborde Celine Texier Dario Sterker Hans-Peter Gschwind Ulrike Pfaar Markus Wartmann Terry M O'Reilly Paul M McSheehy

Anticancer Drugs 2018 08;29(7):691-701

Department of Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland.

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August 2018

2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4.

Authors:
Thomas Knoepfel Pascal Furet Robert Mah Nicole Buschmann Catherine Leblanc Sebastien Ripoche Diana Graus-Porta Markus Wartmann Inga Galuba Robin A Fairhurst

ACS Med Chem Lett 2018 Mar 1;9(3):215-220. Epub 2018 Feb 1.

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

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March 2018

A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.

Authors:
Guido Bold Christian Schnell Pascal Furet Paul McSheehy Josef Brüggen Jürgen Mestan Paul W Manley Peter Drückes Marion Burglin Ursula Dürler Jacqueline Loretan Robert Reuter Markus Wartmann Andreas Theuer Beatrice Bauer-Probst Georg Martiny-Baron Peter Allegrini Arnaud Goepfert Jeanette Wood Amanda Littlewood-Evans

J Med Chem 2016 Jan 21;59(1):132-46. Epub 2015 Dec 21.

Oncology Research, Novartis Institutes for BioMedical Research , 4002 Basel, Switzerland.

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January 2016

CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors.

Authors:
Sadhna R Vora Dejan Juric Nayoon Kim Mari Mino-Kenudson Tiffany Huynh Carlotta Costa Elizabeth L Lockerman Sarah F Pollack Manway Liu Xiaoyan Li Joseph Lehar Marion Wiesmann Markus Wartmann Yan Chen Z Alexander Cao Maria Pinzon-Ortiz Sunkyu Kim Robert Schlegel Alan Huang Jeffrey A Engelman

Cancer Cell 2014 Jul 4;26(1):136-49. Epub 2014 Jul 4.

Massachusetts General Hospital Cancer Center, Boston, MA 02120, USA; Department of Medicine, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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July 2014

The tyrosine phosphatase PTPN14 is a negative regulator of YAP activity.

Authors:
Chrysiis Michaloglou Waltraut Lehmann Typhaine Martin Clara Delaunay Andreas Hueber Louise Barys Honglin Niu Eric Billy Markus Wartmann Moriko Ito Christopher J Wilson Mary Ellen Digan Andreas Bauer Hans Voshol Gerhard Christofori William R Sellers Francesco Hofmann Tobias Schmelzle

PLoS One 2013 16;8(4):e61916. Epub 2013 Apr 16.

Novartis Institutes for BioMedical Research, Disease Area Oncology, Basel, Switzerland.

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November 2013

Acentrosomal spindle organization renders cancer cells dependent on the kinesin HSET.

Authors:
Julia Kleylein-Sohn Bernadette Pöllinger Michaela Ohmer Francesco Hofmann Erich A Nigg Brian A Hemmings Markus Wartmann

J Cell Sci 2012 Nov 3;125(Pt 22):5391-402. Epub 2012 Sep 3.

NIBR Oncology Disease Area, Novartis Pharma AG, CH-4002 Basel, Switzerland.

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November 2012

Anti-cancer activity of 5-O-alkyl 1,4-imino-1,4-dideoxyribitols.

Authors:
Claudia Bello Giovanna Dal Bello Michele Cea Aimable Nahimana Dominique Aubry Anna Garuti Giulia Motta Eva Moran Floriana Fruscione Paolo Pronzato Francesco Grossi Franco Patrone Alberto Ballestrero Marc Dupuis Bernard Sordat Kaspar Zimmermann Jacqueline Loretan Markus Wartmann Michel A Duchosal Alessio Nencioni Pierre Vogel

Bioorg Med Chem 2011 Dec 30;19(24):7720-7. Epub 2011 Jul 30.

Laboratory of Glycochemistry and Asymmetric Synthesis, Swiss Federal Institute of Technology (EPFL), Batochime, CH-1015 Lausanne, Switzerland.

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December 2011

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Authors:
Vito Guagnano Pascal Furet Carsten Spanka Vincent Bordas Mickaël Le Douget Christelle Stamm Josef Brueggen Michael R Jensen Christian Schnell Herbert Schmid Markus Wartmann Joerg Berghausen Peter Drueckes Alfred Zimmerlin Dirksen Bussiere Jeremy Murray Diana Graus Porta

J Med Chem 2011 Oct 21;54(20):7066-83. Epub 2011 Sep 21.

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

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October 2011

A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.

Authors:
Ralph Tiedt Elisa Degenkolbe Pascal Furet Brent A Appleton Sabrina Wagner Joseph Schoepfer Emily Buck David A Ruddy John E Monahan Michael D Jones Jutta Blank Dorothea Haasen Peter Drueckes Markus Wartmann Clive McCarthy William R Sellers Francesco Hofmann

Cancer Res 2011 Aug 22;71(15):5255-64. Epub 2011 Jun 22.

Novartis Institutes for BioMedical Research, Basel, Switzerland.

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August 2011

Natural products as leads for anticancer drug discovery: discovery of new chemotypes of microtubule stabilizers through reengineering of the epothilone scaffold.

Authors:
Karl-Heinz Altmann Frédéric Cachoux Fabian Feyen Jürg Gertsch Christian N Kuzniewski Markus Wartmann

Chimia (Aarau) 2010 ;64(1-2):8-13

"Swiss Federal Institute of Technology (ETH) Zürich Institute of Pharmaceutical Sciences, ETH Hönggerberg, HCI H 405, CH-8093 Zürich.

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February 2011

Evaluation of the mTOR inhibitor, everolimus, in combination with cytotoxic antitumor agents using human tumor models in vitro and in vivo.

Authors:
Terry O'Reilly Paul M J McSheehy Markus Wartmann Peter Lassota Ralf Brandt Heidi A Lane

Anticancer Drugs 2011 Jan;22(1):58-78

Oncology Research, Novartis Institutes for Biomedical Research, Basel, Switzerland.

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January 2011

Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.

Authors:
Paul W Manley Nikolaus Stiefl Sandra W Cowan-Jacob Susan Kaufman Jürgen Mestan Markus Wartmann Marion Wiesmann Richard Woodman Neil Gallagher

Bioorg Med Chem 2010 Oct 14;18(19):6977-86. Epub 2010 Aug 14.

Novartis Institutes for BioMedical Research, Basel, Switzerland.

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October 2010