Publications by authors named "Peter Drueckes"

20Publications

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.

View Article and Find Full Text PDF
January 2021

Promiscuity analysis of a kinase panel screen with designated p38 alpha inhibitors.

Authors:
Mariana González-Medina Filip Miljković Gernot S Haase Peter Drueckes Joerg Trappe Stefan Laufer Jürgen Bajorath

Eur J Med Chem 2020 Feb 20;187:112004. Epub 2019 Dec 20.

Department of Life Science Informatics, B-IT, LIMES Program Unit Chemical Biology and Medicinal Chemistry, Rheinische Friedrich-Wilhelms-Universität, Endenicher Allee 19c, D-53115, Bonn, Germany. Electronic address:

View Article and Find Full Text PDF
February 2020

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.

View Article and Find Full Text PDF
September 2018

Discovery and Characterization of Allosteric WNK Kinase Inhibitors.

Authors:
Ken Yamada Ji-Hu Zhang Xiaoling Xie Juergen Reinhardt Amy Qiongshu Xie Daniel LaSala Darcy Kohls David Yowe Debra Burdick Hajime Yoshisue Hiromichi Wakai Isabel Schmidt Jason Gunawan Kayo Yasoshima Q Kimberley Yue Mitsunori Kato Muneto Mogi Neeraja Idamakanti Natasha Kreder Peter Drueckes Pramod Pandey Toshio Kawanami Waanjeng Huang Yukiko I Yagi Zhan Deng Hyi-Man Park

ACS Chem Biol 2016 12 19;11(12):3338-3346. Epub 2016 Oct 19.

Novartis Institutes for BioMedical Research, Inc. , Cambridge, Massachusetts 02139-4133, United States.

View Article and Find Full Text PDF
December 2016

Protein Kinase Selectivity Profiling Using Microfluid Mobility Shift Assays.

Authors:
Peter Drueckes

Methods Mol Biol 2016 ;1439:143-57

CPC Screening Sciences, Novartis Pharma AG, Novartis Institutes for Biomedical Research, 4002, Basel, Switzerland.

View Article and Find Full Text PDF
December 2017

Type II Inhibitors Targeting CDK2.

Authors:
Leila T Alexander Henrik Möbitz Peter Drueckes Pavel Savitsky Oleg Fedorov Jonathan M Elkins Charlotte M Deane Sandra W Cowan-Jacob Stefan Knapp

ACS Chem Biol 2015 Sep 20;10(9):2116-25. Epub 2015 Jul 20.

Structural Genomics Consortium, University of Oxford , Old Road Campus Research Building, Roosevelt Drive, Oxford, OX3 7DQ, United Kingdom.

View Article and Find Full Text PDF
September 2015

Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers.

Authors:
Pablo D Garcia John L Langowski Yingyun Wang Min Chen Joseph Castillo Christie Fanton Marjorie Ison Tatiana Zavorotinskaya Yumin Dai Jing Lu Xiao-Hong Niu Stephen Basham Julie Chan Jianjun Yu Michael Doyle Paul Feucht Robert Warne Jamie Narberes Tiffany Tsang Christine Fritsch Audrey Kauffmann Estelle Pfister Peter Drueckes Joerg Trappe Christopher Wilson Wooseok Han Jiong Lan Gisele Nishiguchi Mika Lindvall Cornelia Bellamacina J Alex Aycinena Richard Zang Jocelyn Holash Matthew T Burger

Clin Cancer Res 2014 Apr 28;20(7):1834-45. Epub 2014 Jan 28.

Authors' Affiliations: Oncology Disease Area Research; Global Discovery Chemistry/Oncology and Exploratory Chemistry; MAP Group; Chemical and Pharmaceutical Profiling Group, Novartis Institutes for Biomedical Research, Emeryville, California; Developmental Molecular Pathways, Novartis Institutes for Biomedical Research, Cambridge, Massachusetts; Oncology Disease Area Research; and Center for Proteomic Chemistry, Novartis Institutes for Biomedical Research, Basel, Switzerland.

View Article and Find Full Text PDF
April 2014

The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: a proof-of-concept study.

Authors:
Julien Chapelat Frédéric Berst Andreas L Marzinzik Henrik Moebitz Peter Drueckes Joerg Trappe Doriano Fabbro Dieter Seebach

Eur J Med Chem 2012 Nov 4;57:1-9. Epub 2012 Sep 4.

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

View Article and Find Full Text PDF
November 2012

Substrate profiling of IGF-1R and InsR: identification of a potent pentamer substrate.

Authors:
Julien Chapelat Frédéric Berst Andreas L Marzinzik Henrik Moebitz Peter Drueckes Doriano Fabbro Joerg Trappe Dieter Seebach

Bioorg Med Chem Lett 2011 Dec 29;21(23):7030-3. Epub 2011 Sep 29.

Novartis Institutes for BioMedical Research, Basel, Switzerland.

View Article and Find Full Text PDF
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.

View Article and Find Full Text PDF
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.

View Article and Find Full Text PDF
August 2011

Kinase inhibition by deoxy analogues of the resorcylic lactone L-783277.

Authors:
Marc Liniger Christian Neuhaus Tatjana Hofmann Luca Fransioli-Ignazio Michel Jordi Peter Drueckes Jörg Trappe Doriano Fabbro Karl-Heinz Altmann

ACS Med Chem Lett 2011 Jan 20;2(1):22-7. Epub 2010 Oct 20.

Swiss Federal Institute of Technology (ETH) Zurich, Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, 8093 Zurich, Switzerland.

View Article and Find Full Text PDF
January 2011

A fluorescence lifetime-based assay for abelson kinase.

Authors:
Stephan Pritz Gabriele Meder Klaus Doering Peter Drueckes Julian Woelcke Lorenz M Mayr Ulrich Hassiepen

J Biomol Screen 2011 Jan 8;16(1):65-72. Epub 2010 Dec 8.

Biosyntan GmbH, Berlin, Germany.

View Article and Find Full Text PDF
January 2011

Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.

Authors:
Fabienne Baffert Catherine H Régnier Alain De Pover Carole Pissot-Soldermann Gisele A Tavares Francesca Blasco Josef Brueggen Patrick Chène Peter Drueckes Dirk Erdmann Pascal Furet Marc Gerspacher Marc Lang David Ledieu Lynda Nolan Stephan Ruetz Joerg Trappe Eric Vangrevelinghe Markus Wartmann Lorenza Wyder Francesco Hofmann Thomas Radimerski

Mol Cancer Ther 2010 Jul 29;9(7):1945-55. Epub 2010 Jun 29.

Disease Area Oncology, Novartis Institutes for BioMedical Research, 4057 Basel, Switzerland.

View Article and Find Full Text PDF
July 2010

Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.

Authors:
Carole Pissot-Soldermann Marc Gerspacher Pascal Furet Christoph Gaul Philipp Holzer Clive McCarthy Thomas Radimerski Catherine H Regnier Fabienne Baffert Peter Drueckes Gisele A Tavares Eric Vangrevelinghe Francesca Blasco Giorgio Ottaviani Flavio Ossola Julien Scesa Janitha Reetz

Bioorg Med Chem Lett 2010 Apr 19;20(8):2609-13. Epub 2010 Feb 19.

Novartis Institutes for Biomedical Research, Novartis Pharma AG, WKL-136.4.96, CH-4002 Basel, Switzerland.

View Article and Find Full Text PDF
April 2010

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

Authors:
Marc Gerspacher Pascal Furet Carole Pissot-Soldermann Christoph Gaul Philipp Holzer Eric Vangrevelinghe Marc Lang Dirk Erdmann Thomas Radimerski Catherine H Regnier Patrick Chene Alain De Pover Francesco Hofmann Fabienne Baffert Thomas Buhl Reiner Aichholz Francesca Blasco Ralf Endres Jörg Trappe Peter Drueckes

Bioorg Med Chem Lett 2010 Mar 21;20(5):1724-7. Epub 2010 Jan 21.

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

View Article and Find Full Text PDF
March 2010

Extended kinase profile and properties of the protein kinase inhibitor nilotinib.

Authors:
Paul W Manley Peter Drueckes Gabriele Fendrich Pascal Furet Janis Liebetanz Georg Martiny-Baron Jürgen Mestan Jörg Trappe Markus Wartmann Doriano Fabbro

Biochim Biophys Acta 2010 Mar 14;1804(3):445-53. Epub 2009 Nov 14.

Novartis Institutes for Biomedical Research, Basel, Switzerland.

View Article and Find Full Text PDF
March 2010

Affinity classification of kinase inhibitors by mass spectrometric methods and validation using standard IC(50) measurements.

Authors:
Matthias Conradin Jecklin David Touboul Rishi Jain Estee Naggar Toole John Tallarico Peter Drueckes Paul Ramage Renato Zenobi

Anal Chem 2009 Jan;81(1):408-19

Department of Chemistry and Applied Biosciences, ETH Zurich, CH-8093 Zürich, Switzerland.

View Article and Find Full Text PDF
January 2009

Characterization of compound 584, an Abl kinase inhibitor with lasting effects.

Authors:
Miriam Puttini Sara Redaelli Loris Moretti Stefania Brussolo Rosalind H Gunby Luca Mologni Edoardo Marchesi Loredana Cleris Arianna Donella-Deana Peter Drueckes Elisa Sala Vittorio Lucchini Michael Kubbutat Franca Formelli Alfonso Zambon Leonardo Scapozza Carlo Gambacorti-Passerini

Haematologica 2008 May 26;93(5):653-61. Epub 2008 Mar 26.

School of Pharmaceutical Sciences, University of Geneva, Quai Ernest-Ansermet 30, 1211 Genève 4, Switzerland.

View Article and Find Full Text PDF
May 2008

Meriolins, a new class of cell death inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases.

Authors:
Karima Bettayeb Oscar M Tirado Séverine Marionneau-Lambot Yoan Ferandin Olivier Lozach Jonathan C Morris Silvia Mateo-Lozano Peter Drueckes Christoph Schächtele Michael H G Kubbutat François Liger Bernard Marquet Benoît Joseph Aude Echalier Jane A Endicott Vicente Notario Laurent Meijer

Cancer Res 2007 Sep;67(17):8325-34

Centre National de la Recherche Scientifique, Cell Cycle Group & UPS2682, Station Biologique, Roscoff, Bretagne, France.

View Article and Find Full Text PDF
September 2007