Vito Guagnano

BET bromodomain inhibitors regulate keratinocyte plasticity.

Authors:

Gabi Schutzius Christian Kolter Sebastian Bergling Federico Tortelli Florian Fuchs Steffen Renner Vito Guagnano Simona Cotesta Heinrich Rueeger Michael Faller Laure Bouchez Adrian Salathe Florian Nigsch Shola M Richards Malvina Louis Viktoria Gruber Alexandra Aebi Jonathan Turner Frederic Grandjean Jun Li Chris Dimitri Jason R Thomas Markus Schirle Jutta Blank Peter Drueckes Andrea Vaupel Ralph Tiedt Paul W Manley Julia Klopp Rene Hemmig Florence Zink Nelly Leroy Walter Carbone Guglielmo Roma Caroline Gubser Keller Natalie Dales Armin Beyerbach Alfred Zimmerlin Debora Bonenfant Remi Terranova Amy Berwick Sukhdeep Sahambi Aimee Reynolds Lori L Jennings Heinz Ruffner Peter Tarsa Tewis Bouwmeester Vickie Driver Mathias Frederiksen Felix Lohmann Susan Kirkland

Nat Chem Biol 2021 Jan 18. Epub 2021 Jan 18.

Novartis Institutes for BioMedical Research, Basel, Switzerland.

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January 2021

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

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

Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.

Authors:

Robin A Fairhurst Giorgio Caravatti Vito Guagnano Reiner Aichholz Joachim Blanz Francesca Blasco Peter Wipfli Christine Fritsch Sauveur-Michel Maira Christian Schnell Frank H Seiler

Bioorg Med Chem Lett 2016 10 17;26(19):4729-4734. Epub 2016 Aug 17.

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

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October 2016

Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.

Authors:

Pascal Furet Keiichi Masuya Joerg Kallen Thérèse Stachyra-Valat Stephan Ruetz Vito Guagnano Philipp Holzer Robert Mah Stefan Stutz Andrea Vaupel Patrick Chène Sébastien Jeay Achim Schlapbach

Bioorg Med Chem Lett 2016 10 9;26(19):4837-4841. Epub 2016 Aug 9.

Novartis Institutes for BioMedical Research, WKL-136.P.12, CH-4002 Basel, Switzerland.

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October 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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April 2016

Fibroblast growth factor receptors as novel therapeutic targets in SNF5-deleted malignant rhabdoid tumors.

Authors:

Simon Wöhrle Andreas Weiss Moriko Ito Audrey Kauffmann Masato Murakami Zainab Jagani Anne Thuery Beatrice Bauer-Probst Flavia Reimann Christelle Stamm Astrid Pornon Vincent Romanet Vito Guagnano Thomas Brümmendorf William R Sellers Francesco Hofmann Charles W M Roberts Diana Graus Porta

PLoS One 2013 30;8(10):e77652. Epub 2013 Oct 30.

Novartis Institutes for BioMedical Research, Basel, Switzerland.

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August 2014

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Authors:

Pascal Furet Vito Guagnano Robin A Fairhurst Patricia Imbach-Weese Ian Bruce Mark Knapp Christine Fritsch Francesca Blasco Joachim Blanz Reiner Aichholz Jacques Hamon Doriano Fabbro Giorgio Caravatti

Bioorg Med Chem Lett 2013 Jul 14;23(13):3741-8. Epub 2013 May 14.

Novartis Institutes for BioMedical Research, WKL-136.4.12, CH-4002 Basel, Switzerland.

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July 2013

Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets.

Authors:

Simon Wöhrle Christine Henninger Olivier Bonny Anne Thuery Noemie Beluch Nancy E Hynes Vito Guagnano William R Sellers Francesco Hofmann Michaela Kneissel Diana Graus Porta

J Bone Miner Res 2013 Apr;28(4):899-911

Novartis Institutes for BioMedical Research, Basel, Switzerland.

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April 2013

FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor.

Cancer Discov 2012 Dec 20;2(12):1118-33. Epub 2012 Sep 20.

Global Discovery Chemistry, 2Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland.

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December 2012

Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth.

Cancer Discov 2012 Oct 8;2(10):948-59. Epub 2012 Aug 8.

Developmental and Molecular Pathways, Novartis Institutes for BioMedical Research, Cambridge, Massachusetts, USA.

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October 2012

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

Entry into a new class of protein kinase inhibitors by pseudo ring design.

Authors:

Pascal Furet Giorgio Caravatti Vito Guagnano Marc Lang Thomas Meyer Joseph Schoepfer

Bioorg Med Chem Lett 2008 Feb 14;18(3):897-900. Epub 2008 Jan 14.

Novartis Institutes for BioMedical Research, WKL-136.P.12, CH-4002 Basel, Switzerland.

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February 2008

Novel beta-lactam derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome.

Authors:

Patricia Imbach Marc Lang Carlos García-Echeverría Vito Guagnano Maria Noorani Johannes Roesel Francis Bitsch Grety Rihs Pascal Furet

Bioorg Med Chem Lett 2007 Jan 24;17(2):358-62. Epub 2006 Oct 24.

Novartis Institutes for BioMedical Research, WKL-136.4.25, CH-4002 Basel, Switzerland.

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January 2007

Aromatic interactions with phenylalanine 691 and cysteine 828: a concept for FMS-like tyrosine kinase-3 inhibition. Application to the discovery of a new class of potential antileukemia agents.

Authors:

Pascal Furet Guido Bold Thomas Meyer Johannes Roesel Vito Guagnano

J Med Chem 2006 Jul;49(15):4451-4

Novartis Pharma AG, Novartis Institutes for Biomedical Research, CH-4002 Basel, Switzerland.

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July 2006

Entry into a new class of potent proteasome inhibitors having high antiproliferative activity by structure-based design.

Authors:

Pascal Furet Patricia Imbach Maria Noorani Juergen Koeppler Kurt Laumen Marc Lang Vito Guagnano Peter Fuerst Johannes Roesel Johann Zimmermann Carlos García-Echeverría

J Med Chem 2004 Sep;47(20):4810-3

Novartis Pharma AG, Novartis Institutes for Biomedical Research, CH-4002 Basel, Switzerland.

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September 2004

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