Publications by authors named "Pascal Furet"

84Publications

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

A new perspective on the interaction between the Vg/VGLL1-3 proteins and the TEAD transcription factors.

Authors:
Yannick Mesrouze Gustavo Aguilar Fedir Bokhovchuk Typhaine Martin Clara Delaunay Frédéric Villard Marco Meyerhofer Catherine Zimmermann Patrizia Fontana Roman Wille Thomas Vorherr Dirk Erdmann Pascal Furet Clemens Scheufler Tobias Schmelzle Markus Affolter Patrick Chène

Sci Rep 2020 10 15;10(1):17442. Epub 2020 Oct 15.

Disease Area Oncology, Novartis Institutes for Biomedical Research, Novartis, WSJ 386 4.02.01, 4002, Basel, Switzerland.

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October 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

Identification of FAM181A and FAM181B as new interactors with the TEAD transcription factors.

Authors:
Fedir Bokhovchuk Yannick Mesrouze Clara Delaunay Typhaine Martin Frédéric Villard Marco Meyerhofer Patrizia Fontana Catherine Zimmermann Dirk Erdmann Pascal Furet Clemens Scheufler Tobias Schmelzle Patrick Chène

Protein Sci 2020 02 20;29(2):509-520. Epub 2019 Nov 20.

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

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February 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

Structure-based design of potent linear peptide inhibitors of the YAP-TEAD protein-protein interaction derived from the YAP omega-loop sequence.

Authors:
Pascal Furet Bahaa Salem Yannick Mesrouze Tobias Schmelzle Ian Lewis Joerg Kallen Patrick Chène

Bioorg Med Chem Lett 2019 08 18;29(16):2316-2319. Epub 2019 Jun 18.

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

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August 2019

Structural States of Hdm2 and HdmX: X-ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes.

Authors:
Joerg Kallen Aude Izaac Suzanne Chau Emmanuelle Wirth Joseph Schoepfer Robert Mah Achim Schlapbach Stefan Stutz Andrea Vaupel Vito Guagnano Keiichi Masuya Therese-Marie Stachyra Bahaa Salem Patrick Chene Francois Gessier Philipp Holzer Pascal Furet

ChemMedChem 2019 07 27;14(14):1305-1314. Epub 2019 May 27.

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.

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July 2019

Molecular and structural characterization of a TEAD mutation at the origin of Sveinsson's chorioretinal atrophy.

Authors:
Fedir Bokhovchuk Yannick Mesrouze Aude Izaac Marco Meyerhofer Catherine Zimmermann Patrizia Fontana Tobias Schmelzle Dirk Erdmann Pascal Furet Joerg Kallen Patrick Chène

FEBS J 2019 06 11;286(12):2381-2398. Epub 2019 Apr 11.

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

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June 2019

Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation.

Authors:
Sabrina Baltschukat Barbara Schacher Engstler Alan Huang Huai-Xiang Hao Angela Tam Hui Qin Wang Jinsheng Liang Matthew T DiMare Hyo-Eun Carrie Bhang Youzhen Wang Pascal Furet William R Sellers Francesco Hofmann Joseph Schoepfer Ralph Tiedt

Clin Cancer Res 2019 05 23;25(10):3164-3175. Epub 2019 Jan 23.

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

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May 2019

In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.

Authors:
Andrea Vaupel Philipp Holzer Stephane Ferretti Vito Guagnano Joerg Kallen Robert Mah Keiichi Masuya Stephan Ruetz Caroline Rynn Achim Schlapbach Thérèse Stachyra Stefan Stutz Milen Todorov Sébastien Jeay Pascal Furet

Bioorg Med Chem Lett 2018 11 26;28(20):3404-3408. Epub 2018 Aug 26.

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

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November 2018

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

Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.

Authors:
Joseph Schoepfer Wolfgang Jahnke Giuliano Berellini Silvia Buonamici Simona Cotesta Sandra W Cowan-Jacob Stephanie Dodd Peter Drueckes Doriano Fabbro Tobias Gabriel Jean-Marc Groell Robert M Grotzfeld A Quamrul Hassan Chrystèle Henry Varsha Iyer Darryl Jones Franco Lombardo Alice Loo Paul W Manley Xavier Pellé Gabriele Rummel Bahaa Salem Markus Warmuth Andrew A Wylie Thomas Zoller Andreas L Marzinzik Pascal Furet

J Med Chem 2018 09 7;61(18):8120-8135. Epub 2018 Sep 7.

Novartis Institutes for BioMedical Research, Novartis Campus , CH-4056 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

Adaptation of the bound intrinsically disordered protein YAP to mutations at the YAP:TEAD interface.

Authors:
Yannick Mesrouze Fedir Bokhovchuk Aude Izaac Marco Meyerhofer Catherine Zimmermann Patrizia Fontana Tobias Schmelzle Dirk Erdmann Pascal Furet Joerg Kallen Patrick Chène

Protein Sci 2018 10;27(10):1810-1820

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

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October 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

Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.

Authors:
Robin A Fairhurst Thomas Knoepfel Catherine Leblanc Nicole Buschmann Christoph Gaul Jutta Blank Inga Galuba Jörg Trappe Chao Zou Johannes Voshol Christine Genick Peggy Brunet-Lefeuvre Francis Bitsch Diana Graus-Porta Pascal Furet

Medchemcomm 2017 Aug 8;8(8):1604-1613. Epub 2017 Jun 8.

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

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August 2017

The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.

Authors:
Andrew A Wylie Joseph Schoepfer Wolfgang Jahnke Sandra W Cowan-Jacob Alice Loo Pascal Furet Andreas L Marzinzik Xavier Pelle Jerry Donovan Wenjing Zhu Silvia Buonamici A Quamrul Hassan Franco Lombardo Varsha Iyer Michael Palmer Giuliano Berellini Stephanie Dodd Sanjeev Thohan Hans Bitter Susan Branford David M Ross Timothy P Hughes Lilli Petruzzelli K Gary Vanasse Markus Warmuth Francesco Hofmann Nicholas J Keen William R Sellers

Nature 2017 03 22;543(7647):733-737. Epub 2017 Mar 22.

Novartis Institutes for BioMedical Research, Cambridge, Massachusetts 02139, USA.

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March 2017

Polyclonal Secondary Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion-Positive Cholangiocarcinoma.

Authors:
Lipika Goyal Supriya K Saha Leah Y Liu Giulia Siravegna Ignaty Leshchiner Leanne G Ahronian Jochen K Lennerz Phuong Vu Vikram Deshpande Avinash Kambadakone Benedetta Mussolin Stephanie Reyes Laura Henderson Jiaoyuan Elisabeth Sun Emily E Van Seventer Joseph M Gurski Sabrina Baltschukat Barbara Schacher-Engstler Louise Barys Christelle Stamm Pascal Furet David P Ryan James R Stone A John Iafrate Gad Getz Diana Graus Porta Ralph Tiedt Alberto Bardelli Dejan Juric Ryan B Corcoran Nabeel Bardeesy Andrew X Zhu

Cancer Discov 2017 03 29;7(3):252-263. Epub 2016 Dec 29.

Massachusetts General Hospital Cancer Center, Harvard Medical School, Boston, Massachusetts.

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March 2017

Bioorthogonal Probes for the Study of MDM2-p53 Inhibitors in Cells and Development of High-Content Screening Assays for Drug Discovery.

Authors:
Pier Luca D'Alessandro Nicole Buschmann Markus Kaufmann Pascal Furet Frederic Baysang Reto Brunner Andreas Marzinzik Thomas Vorherr Therese-Marie Stachyra Johannes Ottl Dimitrios E Lizos Amanda Cobos-Correa

Angew Chem Int Ed Engl 2016 12 22;55(52):16026-16030. Epub 2016 Nov 22.

Center for Proteomic Chemistry, Novartis Institutes of Biomedical Research, Novartis Campus, Basel, Switzerland.

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December 2016

Correction: A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097.

Authors:
Sébastien Jeay Swann Gaulis Stéphane Ferretti Hans Bitter Moriko Ito Thérèse Valat Masato Murakami Stephan Ruetz Daniel A Guthy Caroline Rynn Michael R Jensen Marion Wiesmann Joerg Kallen Pascal Furet François Gessier Philipp Holzer Keiichi Masuya Jens Würthner Ensar Halilovic Francesco Hofmann William R Sellers Diana Graus Porta

Elife 2016 11 17;5. Epub 2016 Nov 17.

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November 2016