Wolfgang Jahnke

Summary

Affiliation: Novartis Institutes for BioMedical Research

Publications

  1. ncbi request reprint Spin labels as a tool to identify and characterize protein-ligand interactions by NMR spectroscopy
    Wolfgang Jahnke
    Novartis Pharma AG, WSJ 88 904, P O Box 4002, Basel, Switzerland
    Chembiochem 3:167-73. 2002
  2. ncbi request reprint NMR reporter screening for the detection of high-affinity ligands
    Wolfgang Jahnke
    Novartis Pharma AG, P O Box, 4002 Basel, Switzerland
    Angew Chem Int Ed Engl 41:3420-3. 2002
  3. doi request reprint Backbone NMR resonance assignment of the Abelson kinase domain in complex with imatinib
    Navratna Vajpai
    Biozentrum, University of Basel, Klingelbergstrasse 70, Basel, Switzerland
    Biomol NMR Assign 2:41-2. 2008
  4. doi request reprint An in vitro assay to measure targeted drug delivery to bone mineral
    Wolfgang Jahnke
    Novartis Institutes for BioMedical Research, Center for Proteomic Chemistry, Basel, Switzerland
    ChemMedChem 5:770-6. 2010
  5. ncbi request reprint Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay
    Wolfgang Jahnke
    Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland
    J Am Chem Soc 132:7043-8. 2010
  6. ncbi request reprint Perspectives of biomolecular NMR in drug discovery: the blessing and curse of versatility
    Wolfgang Jahnke
    Novartis Institutes for BioMedical Research, Discovery Technologies, Basel 4002, Switzerland
    J Biomol NMR 39:87-90. 2007
  7. ncbi request reprint Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
    Wolfgang Jahnke
    Center for Proteomic Chemistry and Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Basel, Switzerland
    Nat Chem Biol 6:660-6. 2010
  8. ncbi request reprint Strategies for the NMR-based identification and optimization of allosteric protein kinase inhibitors
    Wolfgang Jahnke
    Novartis Institutes for BioMedical Research, Discovery Technologies, WSJ 88 904, 4002 Basel, Switzerland
    Chembiochem 6:1607-10. 2005
  9. doi request reprint Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site
    Doriano Fabbro
    Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland
    Biochim Biophys Acta 1804:454-62. 2010
  10. ncbi request reprint Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib
    Navratna Vajpai
    Novartis Institutes for BioMedical Research, Basel, Switzerland
    J Biol Chem 283:18292-302. 2008

Detail Information

Publications33

  1. ncbi request reprint Spin labels as a tool to identify and characterize protein-ligand interactions by NMR spectroscopy
    Wolfgang Jahnke
    Novartis Pharma AG, WSJ 88 904, P O Box 4002, Basel, Switzerland
    Chembiochem 3:167-73. 2002
    ..The concept of utilizing spin labels in NMR spectroscopy is summarized, examples for successful first-site and second-site NMR spectroscopic screens are given, and guidelines for linker design are presented...
  2. ncbi request reprint NMR reporter screening for the detection of high-affinity ligands
    Wolfgang Jahnke
    Novartis Pharma AG, P O Box, 4002 Basel, Switzerland
    Angew Chem Int Ed Engl 41:3420-3. 2002
  3. doi request reprint Backbone NMR resonance assignment of the Abelson kinase domain in complex with imatinib
    Navratna Vajpai
    Biozentrum, University of Basel, Klingelbergstrasse 70, Basel, Switzerland
    Biomol NMR Assign 2:41-2. 2008
    ..Here we report the first almost complete backbone assignment of c-ABL kinase domain in complex with imatinib...
  4. doi request reprint An in vitro assay to measure targeted drug delivery to bone mineral
    Wolfgang Jahnke
    Novartis Institutes for BioMedical Research, Center for Proteomic Chemistry, Basel, Switzerland
    ChemMedChem 5:770-6. 2010
    ..This assay supports a strategy for targeted delivery of drugs to bone by attaching a bone-affinity tag to the active drug substance...
  5. ncbi request reprint Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay
    Wolfgang Jahnke
    Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland
    J Am Chem Soc 132:7043-8. 2010
    ..Activation of c-Abl by allosteric agonists has been confirmed in a biochemical assay...
  6. ncbi request reprint Perspectives of biomolecular NMR in drug discovery: the blessing and curse of versatility
    Wolfgang Jahnke
    Novartis Institutes for BioMedical Research, Discovery Technologies, Basel 4002, Switzerland
    J Biomol NMR 39:87-90. 2007
    ....
  7. ncbi request reprint Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
    Wolfgang Jahnke
    Center for Proteomic Chemistry and Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Basel, Switzerland
    Nat Chem Biol 6:660-6. 2010
    ..This allosteric and druggable pocket allows the development of a new generation of FPPS inhibitors that are optimized for direct antitumor effects in soft tissue...
  8. ncbi request reprint Strategies for the NMR-based identification and optimization of allosteric protein kinase inhibitors
    Wolfgang Jahnke
    Novartis Institutes for BioMedical Research, Discovery Technologies, WSJ 88 904, 4002 Basel, Switzerland
    Chembiochem 6:1607-10. 2005
  9. doi request reprint Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site
    Doriano Fabbro
    Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland
    Biochim Biophys Acta 1804:454-62. 2010
    ....
  10. ncbi request reprint Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib
    Navratna Vajpai
    Novartis Institutes for BioMedical Research, Basel, Switzerland
    J Biol Chem 283:18292-302. 2008
    ..Nanosecond as well as microsecond dynamics can be detected for certain residues in the activation loop in the inactive and active conformation complexes...
  11. ncbi request reprint The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation
    Sandra W Cowan-Jacob
    Discovery Technologies, Novartis Institutes for BioMedical Research, CH 4056 Basel, Switzerland
    Structure 13:861-71. 2005
    ..This structure reveals why the drug shows a low affinity for active kinase conformations, contributing to its excellent kinase selectivity profile...
  12. doi request reprint Time efficient detection of protein-ligand interactions with the polarization optimized PO-WaterLOGSY NMR experiment
    Alvar D Gossert
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, 4002, Basel, Switzerland
    J Biomol NMR 43:211-7. 2009
    ..These time savings have a substantial impact in drug discovery, since significantly larger compound libraries can be tested in screening campaigns...
  13. ncbi request reprint Structural basis for the exceptional in vivo efficacy of bisphosphonate drugs
    Jean Michel Rondeau
    Novartis Institutes for BioMedical Research, Discovery Technologies, 4002 Basel, Switzerland
    ChemMedChem 1:267-73. 2006
    ..Moreover, our data form the basis for structure-guided design of optimized N-BPs with improved pharmacological properties...
  14. ncbi request reprint Efficient uniform isotope labeling of Abl kinase expressed in Baculovirus-infected insect cells
    Andre Strauss
    Novartis Institutes for BioMedical Research, Basel, Switzerland
    J Biomol NMR 31:343-9. 2005
    ..The presented isotope labeling method should be applicable also to further proteins where successful expression is restricted to the Baculovirus expression system...
  15. ncbi request reprint NMR resonance assignment of selectively labeled proteins by the use of paramagnetic ligands
    Brian Cutting
    Novartis Institutes of Biomedical Research, P O Box CH 4002, Basel, Switzerland
    J Biomol NMR 30:205-10. 2004
    ..The method is demonstrated for the catalytic domain of Abl kinase in complex with the inhibitor, STI571...
  16. doi request reprint Isotope labeling in insect cells
    Alvar D Gossert
    Novartis Institutes for BioMedical Research, Basel, Switzerland
    Adv Exp Med Biol 992:179-96. 2012
    ..The chapter is concluded with case studies, describing successful application of isotope labeling in insect cells for NMR studies including solid-state experiments, ligand binding studies and protein dynamics...
  17. doi request reprint A simple protocol for amino acid type selective isotope labeling in insect cells with improved yields and high reproducibility
    Alvar D Gossert
    Novartis Institutes for BioMedical Research, Basel, Switzerland
    J Biomol NMR 51:449-56. 2011
    ..We show applications with human kinases, where protein-ligand interactions are characterized by 2D [(15)N, (1)H]- and [(13)C, (1)H]-HSQC spectra...
  18. doi request reprint NMR-Based Strategies to Elucidate Bioactive Conformations of Weakly Binding Ligands
    Marcel J J Blommers
    Novartis Institutes for BioMedical Research, Discovery Technologies, 4002, Basel, Switzerland
    Top Curr Chem 273:1-14. 2008
    ..The application of these techniques will be discussed in detail for a peptide derived fromIKKβ bound to the protein NEMO that plays an important rolein the NFκB pathway...
  19. doi request reprint In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I
    Laszlo Revesz
    Novartis Institutes for BioMedical Research, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 20:4715-8. 2010
    ....
  20. ncbi request reprint NMR and in silico screening
    Simon Rüdisser
    Novartis Pharma AG, 4002, Switzerland
    Comb Chem High Throughput Screen 5:591-603. 2002
    ..We will first give a short overview of existing NMR and in silico screening methods, discuss the drawbacks associated with each, and finally present applications that highlight the combination of the two technologies...
  21. ncbi request reprint Second-site NMR screening and linker design
    Wolfgang Jahnke
    Novartis Pharma AG, Central Technologies and Oncology Research, CH 4002 Basel, Switzerland
    Curr Top Med Chem 3:69-80. 2003
    ..Published examples from second-site screening and linker design are summarized, and are complemented by previously unpublished in-house examples...
  22. ncbi request reprint Library design for fragment based screening
    Ansgar Schuffenhauer
    Novartis Institutes of Biomedical Research, CH 4002 Basel, Switzerland
    Curr Top Med Chem 5:751-62. 2005
    ..For example primary amines can be masked as acetamides. If the screening fragment is active the related building block can then be used for synthesis of a follow-up library...
  23. ncbi request reprint Amino-acid-type selective isotope labeling of proteins expressed in Baculovirus-infected insect cells useful for NMR studies
    Andre Strauss
    Novartis Pharma AG, Central Technologies, Oncology Research, CH 4002 Basel, Switzerland
    J Biomol NMR 26:367-72. 2003
    ..The method should be applicable to amino-acid-type selective isotope labeling of other recombinant proteins which have not been amenable to NMR analysis...
  24. ncbi request reprint The chemistry of bisphosphonates: from antiscaling agents to clinical therapeutics
    Leo Widler
    WKL 136 3 93, Novartis Institutes for BioMedical Research, CH 4057 Basel, Switzerland
    Anticancer Agents Med Chem 12:95-101. 2012
    ....
  25. ncbi request reprint New approaches for NMR screening in drug discovery
    César Fernández
    Novartis Institutes for BioMedical Research, 4002 Basel, Switzerland Electronic
    Drug Discov Today Technol 1:277-83. 2004
    ..These methods have made an appreciable contribution to drug design, leading to the discovery of a large number of high affinity ligands for biologically relevant protein targets.: ..
  26. doi request reprint Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases
    Sandra W Cowan-Jacob
    Novartis Institutes for BioMedical Research, Novartis Campus, CH 4056 Basel, Switzerland
    Future Med Chem 6:541-61. 2014
    ..In this perspective, the opportunities and challenges of following these approaches and others will be discussed. ..
  27. ncbi request reprint Control of intrinsically disordered stathmin by multisite phosphorylation
    Srinivas Honnappa
    Biomolecular Research, Structural Biology, Paul Scherrer Insititut, CH 5232 Villigen PSI, Switzerland
    J Biol Chem 281:16078-83. 2006
    ..The insight into the tubulin-stathmin interaction offers a molecular basis for understanding the nature and the factors that control intrinsically disordered protein systems in general...
  28. ncbi request reprint Thermodynamics of the Op18/stathmin-tubulin interaction
    Srinivas Honnappa
    Structural Biology, Paul Scherrer Institut, CH 5232 Villigen PSI, Switzerland
    J Biol Chem 278:38926-34. 2003
    ..5 compared with pH 6.8. This decrease could be attributed to a weaker binding of the C terminus of stathmin. These findings do not support the view that stathmin works as a pH-sensitive protein...
  29. ncbi request reprint The high-resolution solution structure of epothilone A bound to tubulin: an understanding of the structure-activity relationships for a powerful class of antitumor agents
    Teresa Carlomagno
    Max Planck Institut fur biophysikalische Chemie, Am Fassberg 11, 37 077 Göttingen, Germany
    Angew Chem Int Ed Engl 42:2511-5. 2003
  30. ncbi request reprint Backbone resonance assignment of the 298 amino acid catalytic domain of protein tyrosine phosphatase 1B (PTP1B)
    Sebastian Meier
    J Biomol NMR 24:165-6. 2002
  31. pmc Molecular basis of coiled-coil formation
    Michel O Steinmetz
    Biomolecular Research, Structural Biology, Paul Scherrer Institut, CH 5232 Villigen PSI, Switzerland
    Proc Natl Acad Sci U S A 104:7062-7. 2007
    ..Our findings provide a general explanation for the molecular mechanism of coiled-coil formation...
  32. ncbi request reprint Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors
    Eva Altmann
    J Med Chem 45:2352-4. 2002
    ..Compounds 4b, 4e, and 4g exhibit high potency toward rabbit and human cathepsin K (IC(50) < 0.006 microM) and are characterized by an excellent selectivity profile vs human cathepsins L and S...
  33. ncbi request reprint Molecular-dynamics simulations of C- and N-terminal peptide derivatives of GCN4-p1 in aqueous solution
    John H Missimer
    Biomolecular Research, Paul Scherrer Institut, CH 5232 Villigen
    Chem Biodivers 2:1086-104. 2005
    ..Analysis does not indicate that the N-terminal half is less stable than the C-terminal half, indicating that 100 ns is too short a period to observe complete unfolding...