Juraj Velcicky

Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.

Authors:

Juraj Velcicky Rainer Wilcken Simona Cotesta Philipp Janser Achim Schlapbach Trixie Wagner Philippe Piechon Frederic Villard Rochdi Bouhelal Fabian Piller Stephanie Harlfinger Rowan Stringer Dominique Fehlmann Klemens Kaupmann Amanda Littlewood-Evans Matthias Haffke Nina Gommermann

J Med Chem 2020 09 28;63(17):9856-9875. Epub 2020 Aug 28.

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

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September 2020

The Proton-Sensing GPR4 Receptor Regulates Paracellular Gap Formation and Permeability of Vascular Endothelial Cells.

Authors:

Elizabeth A Krewson Edward J Sanderlin Mona A Marie Shayan Nik Akhtar Juraj Velcicky Pius Loetscher Li V Yang

iScience 2020 Feb 17;23(2):100848. Epub 2020 Jan 17.

Department of Anatomy and Cell Biology, East Carolina University, Greenville, NC 27834, USA; Department of Internal Medicine, Brody School of Medicine, East Carolina University, Greenville, NC 27834, USA. Electronic address:

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February 2020

Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.

Authors:

Juraj Velcicky Casey J N Mathison Victor Nikulin Daniel Pflieger Robert Epple Mihai Azimioara Christopher Cow Pierre-Yves Michellys Pascal Rigollier Daniel R Beisner Ursula Bodendorf Danilo Guerini Bo Liu Ben Wen Samantha Zaharevitz Trixi Brandl

ACS Med Chem Lett 2019 Jun 23;10(6):887-892. Epub 2019 May 23.

Global Discovery Chemistry, and Autoimmunity Transplantation Inflammation, Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.

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June 2019

Pharmacological inhibition of GPR4 remediates intestinal inflammation in a mouse colitis model.

Authors:

Edward J Sanderlin Mona Marie Juraj Velcicky Pius Loetscher Li V Yang

Eur J Pharmacol 2019 Jun 28;852:218-230. Epub 2019 Mar 28.

Department of Internal Medicine, Brody School of Medicine, East Carolina University, USA; Department of Anatomy and Cell Biology, Brody School of Medicine, East Carolina University, USA. Electronic address:

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June 2019

Modulating ADME Properties by Fluorination: MK2 Inhibitors with Improved Oral Exposure.

Authors:

Juraj Velcicky Achim Schlapbach Richard Heng Laszlo Revesz Daniel Pflieger Ernst Blum Stuart Hawtin Christine Huppertz Roland Feifel Rene Hersperger

ACS Med Chem Lett 2018 Apr 20;9(4):392-396. Epub 2018 Mar 20.

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

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April 2018

Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects In Vivo.

Authors:

Juraj Velcicky Ursula Bodendorf Pascal Rigollier Robert Epple Daniel R Beisner Danilo Guerini Philip Smith Bo Liu Roland Feifel Peter Wipfli Reiner Aichholz Philippe Couttet Ina Dix Toni Widmer Ben Wen Trixi Brandl

J Med Chem 2018 02 23;61(3):865-880. Epub 2018 Jan 23.

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

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February 2018

Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis.

Authors:

Wolfgang Miltz Juraj Velcicky Janet Dawson Amanda Littlewood-Evans Marie-Gabrielle Ludwig Klaus Seuwen Roland Feifel Berndt Oberhauser Arndt Meyer Daniela Gabriel Mark Nash Pius Loetscher

Bioorg Med Chem 2017 08 29;25(16):4512-4525. Epub 2017 Jun 29.

Autoimmunity, Transplantation and Inflammation, Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland.

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August 2017

Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis.

Authors:

Juraj Velcicky Wolfgang Miltz Berndt Oberhauser David Orain Andrea Vaupel Klaus Weigand Janet Dawson King Amanda Littlewood-Evans Mark Nash Roland Feifel Pius Loetscher

J Med Chem 2017 05 26;60(9):3672-3683. Epub 2017 Apr 26.

Global Discovery Chemistry, ‡Autoimmunity Transplantation Inflammation, §Musculoskeletal, ∥Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research , CH-4002 Basel, Switzerland.

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May 2017

Nucleoside analogues with a 1,3-diene-Fe(CO)3 substructure: stereoselective synthesis, configurational assignment, and apoptosis-inducing activity.

Authors:

Christoph Hirschhäuser Juraj Velcicky Daniel Schlawe Erik Hessler André Majdalani Jörg-Martin Neudörfl Aram Prokop Thomas Wieder Hans-Günther Schmalz

Chemistry 2013 Sep 9;19(39):13017-29. Epub 2013 Aug 9.

Department of Chemistry, University of Cologne, Greinstrasse 4, 50939 Köln (Germany), Fax: (+49) 221-470-3064.

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September 2013

Palladium-catalyzed cyanomethylation of aryl halides through domino Suzuki coupling-isoxazole fragmentation.

Authors:

Juraj Velcicky Arne Soicke Roland Steiner Hans-Günther Schmalz

J Am Chem Soc 2011 May 19;133(18):6948-51. Epub 2011 Apr 19.

Novartis Institutes for Biomedical Research, Forum 1, Novartis Campus, CH-4056 Basel, Switzerland.

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May 2011

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.

Authors:

Laszlo Revesz Achim Schlapbach Reiner Aichholz Roland Feifel Stuart Hawtin Richard Heng Peter Hiestand Wolfgang Jahnke Guido Koch Markus Kroemer Henrik Möbitz Clemens Scheufler Juraj Velcicky Christine Huppertz

Bioorg Med Chem Lett 2010 Aug 13;20(15):4715-8. Epub 2010 Apr 13.

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

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August 2010

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.

Authors:

Laszlo Revesz Achim Schlapbach Reiner Aichholz Janet Dawson Roland Feifel Stuart Hawtin Amanda Littlewood-Evans Guido Koch Markus Kroemer Henrik Möbitz Clemens Scheufler Juraj Velcicky Christine Huppertz

Bioorg Med Chem Lett 2010 Aug 11;20(15):4719-23. Epub 2010 Apr 11.

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

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August 2010

Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.

Authors:

Juraj Velcicky Roland Feifel Stuart Hawtin Richard Heng Christine Huppertz Guido Koch Markus Kroemer Henrik Moebitz Laszlo Revesz Clemens Scheufler Achim Schlapbach

Bioorg Med Chem Lett 2010 Feb 3;20(3):1293-7. Epub 2009 Nov 3.

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

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February 2010

Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.

Authors:

Achim Schlapbach Roland Feifel Stuart Hawtin Richard Heng Guido Koch Henrik Moebitz Laszlo Revesz Clemens Scheufler Juraj Velcicky Rudolf Waelchli Christine Huppertz

Bioorg Med Chem Lett 2008 Dec 11;18(23):6142-6. Epub 2008 Oct 11.

Novartis Institutes for BioMedical Research, global Discovery Chemistry, WSJ-88.508, CH-4002 Basel, Switzerland.

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December 2008

Total synthesis of (-)- and ent-(+)-vindoline and related alkaloids.

Authors:

Hayato Ishikawa Gregory I Elliott Juraj Velcicky Younggi Choi Dale L Boger

J Am Chem Soc 2006 Aug;128(32):10596-612

Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.

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August 2006