Ulrich Hassiepen

Summary

Affiliation: Novartis Institutes for BioMedical Research

Publications

  1. ncbi request reprint A sensitive fluorescence intensity assay for deubiquitinating proteases using ubiquitin-rhodamine110-glycine as substrate
    Ulrich Hassiepen
    Novartis Institutes for BioMedical Research, Center for Proteomic Chemistry Expertise Platform Proteases, Novartis Pharma AG, 4002 Basel, Switzerland
    Anal Biochem 371:201-7. 2007
  2. doi request reprint The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches
    Edwige Lorthiois
    Novartis Pharma AG, Institutes for Biomedical Research, Novartis Campus, CH 4056 Basel, Switzerland
    J Med Chem 56:2207-17. 2013
  3. doi request reprint Fluorescence Lifetime-Based Competitive Binding Assays for Measuring the Binding Potency of Protease Inhibitors In Vitro
    Andreas Boettcher
    Novartis Institutes for Biomedical Research NIBR, Expertise Platform Proteases, Novartis Pharma AG, Basel, Switzerland
    J Biomol Screen 19:870-7. 2014
  4. pmc Targeted inhibition of the COP9 signalosome for treatment of cancer
    Anita Schlierf
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, 4002 Basel, Switzerland
    Nat Commun 7:13166. 2016
  5. ncbi request reprint Multi-photon excitation of intrinsic protein fluorescence and its application to pharmaceutical drug screening
    Christof Buehler
    Discovery Technologies Innovative Screening Technologies, Novartis Institutes for BioMedical Research GmbH and Co KG, Vienna, Austria
    Assay Drug Dev Technol 3:155-67. 2005
  6. ncbi request reprint Crystal structure of human BACE2 in complex with a hydroxyethylamine transition-state inhibitor
    Nils Ostermann
    Protease Platform, Novartis Institutes for BioMedical Research, CH 4002 Basel, Switzerland
    J Mol Biol 355:249-61. 2006
  7. doi request reprint A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore
    Nils Ostermann
    Novartis Pharma AG, Institutes for Biomedical Research, Novartis Campus, CH 4056 Basel, Switzerland
    J Med Chem 56:2196-206. 2013
  8. pmc A macrocyclic HCV NS3/4A protease inhibitor interacts with protease and helicase residues in the complex with its full-length target
    Nikolaus Schiering
    Expertise Platform Proteases, Novartis Institutes for BioMedical Research, Fabrikstrasse 16, CH 4002 Basel, Switzerland
    Proc Natl Acad Sci U S A 108:21052-6. 2011
  9. doi request reprint Fragment-based screening by biochemical assays: Systematic feasibility studies with trypsin and MMP12
    Andreas Boettcher
    Novartis Institutes for BioMedical Research, Expertise Platform Proteases, Novartis Pharma AG, Basel, Switzerland
    J Biomol Screen 15:1029-41. 2010
  10. doi request reprint The crystal structure of caspase-6, a selective effector of axonal degeneration
    Renato Baumgartner
    Novartis Institutes for BioMedical Research, Center for Proteomic Chemistry, Expertise Platform Proteases, 4002 Basel, Switzerland
    Biochem J 423:429-39. 2009

Collaborators

  • Martin Renatus
  • Allan D'arcy
  • Eva Altmann
  • Martin Klumpp
  • Lorenz M Mayr
  • Nikolaus Schiering
  • Edgar Jacoby
  • Andreas Weiss
  • Nils Ostermann
  • Andreas Boettcher
  • Edwige Lorthiois
  • Frederic Cumin
  • Jürgen Maibaum
  • Anita Schlierf
  • Richard Sedrani
  • Eric Francotte
  • Trixie Wagner
  • Dean F Rigel
  • Claus Ehrhardt
  • Takatoshi Kosaka
  • Werner Breitenstein
  • Paul Richert
  • Randy L Webb
  • Julian Woelcke
  • Simon Ruedisser
  • Jörg Eder
  • Bernd Gerhartz
  • Renato Baumgartner
  • Christof Buehler
  • Michael Kiffe
  • Bruno Martoglio
  • Michael Schaefer
  • Anne B Jefferson
  • Jean Quancard
  • Rene Assenberg
  • Matthew Jones
  • Christian Wiesmann
  • David Orain
  • Trixi Brandl
  • Nathalie Gradoux
  • Andreas Marzinzik
  • Sabine Geisse
  • Daniel K Baeschlin
  • Markus Kromer
  • Johannes Ottl
  • Jörg Trappe
  • J Constanze D Hartwieg
  • Eric Vangrevelinghe
  • Holger Sellner
  • Daniela Vinzenz
  • Pascal Rigollier
  • Paulus Erbel
  • Gabriele Meder
  • Arnaud Decock
  • Christophe Briand
  • Richard Morse
  • Ulf Eidhoff
  • Susanne Worpenberg
  • Ulrich Hommel
  • Florence Zink
  • Oliver Simic
  • Alain Schilb
  • Kurt A Stoeckli
  • Kurt Mueller
  • Peter T C So
  • Joerg Dreessen
  • Manfred Auer

Detail Information

Publications12

  1. ncbi request reprint A sensitive fluorescence intensity assay for deubiquitinating proteases using ubiquitin-rhodamine110-glycine as substrate
    Ulrich Hassiepen
    Novartis Institutes for BioMedical Research, Center for Proteomic Chemistry Expertise Platform Proteases, Novartis Pharma AG, 4002 Basel, Switzerland
    Anal Biochem 371:201-7. 2007
    ..Due to the low protease concentrations and high sensitivity, this assay would allow the determination of inhibitory constants in the subnanomolar range...
  2. doi request reprint The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches
    Edwige Lorthiois
    Novartis Pharma AG, Institutes for Biomedical Research, Novartis Campus, CH 4056 Basel, Switzerland
    J Med Chem 56:2207-17. 2013
    ..The prototype analogue (3S,4S)-12a of this new class of direct renin inhibitors exerted blood pressure lowering effects in a hypertensive double-transgenic rat model after oral administration...
  3. doi request reprint Fluorescence Lifetime-Based Competitive Binding Assays for Measuring the Binding Potency of Protease Inhibitors In Vitro
    Andreas Boettcher
    Novartis Institutes for Biomedical Research NIBR, Expertise Platform Proteases, Novartis Pharma AG, Basel, Switzerland
    J Biomol Screen 19:870-7. 2014
    ....
  4. pmc Targeted inhibition of the COP9 signalosome for treatment of cancer
    Anita Schlierf
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, 4002 Basel, Switzerland
    Nat Commun 7:13166. 2016
    ..Our results provide insights into how CSN regulates CRLs and suggest that CSN5 inhibition has potential for anti-tumour therapy...
  5. ncbi request reprint Multi-photon excitation of intrinsic protein fluorescence and its application to pharmaceutical drug screening
    Christof Buehler
    Discovery Technologies Innovative Screening Technologies, Novartis Institutes for BioMedical Research GmbH and Co KG, Vienna, Austria
    Assay Drug Dev Technol 3:155-67. 2005
    ..By using the intrinsic fluorescence intensity of a protein-substrate, we were able to discriminate between ligands of different affinities in binding assays...
  6. ncbi request reprint Crystal structure of human BACE2 in complex with a hydroxyethylamine transition-state inhibitor
    Nils Ostermann
    Protease Platform, Novartis Institutes for BioMedical Research, CH 4002 Basel, Switzerland
    J Mol Biol 355:249-61. 2006
    ....
  7. doi request reprint A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore
    Nils Ostermann
    Novartis Pharma AG, Institutes for Biomedical Research, Novartis Campus, CH 4056 Basel, Switzerland
    J Med Chem 56:2196-206. 2013
    ..3S,5R)-12 showed oral bioavailability in rats and demonstrated blood pressure lowering activity in the double-transgenic rat model...
  8. pmc A macrocyclic HCV NS3/4A protease inhibitor interacts with protease and helicase residues in the complex with its full-length target
    Nikolaus Schiering
    Expertise Platform Proteases, Novartis Institutes for BioMedical Research, Fabrikstrasse 16, CH 4002 Basel, Switzerland
    Proc Natl Acad Sci U S A 108:21052-6. 2011
    ..In addition, small angle X-ray scattering confirmed the observed protease-helicase domain assembly in solution...
  9. doi request reprint Fragment-based screening by biochemical assays: Systematic feasibility studies with trypsin and MMP12
    Andreas Boettcher
    Novartis Institutes for BioMedical Research, Expertise Platform Proteases, Novartis Pharma AG, Basel, Switzerland
    J Biomol Screen 15:1029-41. 2010
    ..Extrapolated to 10,000 fragments, the biochemical assays speed up the primary FBS process by approximately a factor of 10 and reduce the protease consumption by approximately 10,000-fold compared to NMR protein observation experiments...
  10. doi request reprint The crystal structure of caspase-6, a selective effector of axonal degeneration
    Renato Baumgartner
    Novartis Institutes for BioMedical Research, Center for Proteomic Chemistry, Expertise Platform Proteases, 4002 Basel, Switzerland
    Biochem J 423:429-39. 2009
    ..However, targeting the latent conformation in search for specific and bio-available caspase-6 inhibitors might offer an alternative to active-site-directed approaches...
  11. ncbi request reprint Structural basis of ubiquitin recognition by the deubiquitinating protease USP2
    Martin Renatus
    Protease Platform, Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland
    Structure 14:1293-302. 2006
    ..As several of those molecules are found at identical positions in the previously solved USP7/ubiquitin-aldehyde complex structure, we suggest a general mechanism of water-mediated ubiquitin recognition by USPs...
  12. doi request reprint Azaindoles as Zinc-Binding Small-Molecule Inhibitors of the JAMM Protease CSN5
    Eva Altmann
    Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland
    Angew Chem Int Ed Engl . 2016
    ..The best compounds inhibited CSN5 with nanomolar potency, led to degradation of the substrate recognition subunit Skp2 in cells, and reduced the viability of HCT116 cells...