Jean Michel Rondeau

Summary

Affiliation: Novartis Institutes for BioMedical Research

Publications

  1. ncbi request reprint Structure-based design and protein X-ray analysis of a protein kinase inhibitor
    Pascal Furet
    Novartis Pharmaceuticals Inc, Oncology Research, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 12:221-4. 2002
  2. 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
  3. doi 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
  4. doi request reprint Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application
    Andreas Lerchner
    Novartis Institutes for BioMedicalResearch, Novartis Pharma AG, PO Box, CH 4002, Basel, Switzerland
    Bioorg Med Chem Lett 20:603-7. 2010
  5. doi request reprint Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors
    Rainer Machauer
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, PO Box, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 19:1361-5. 2009
  6. doi request reprint Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors
    Heinrich Rueeger
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, PO Box, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 21:1942-7. 2011
  7. doi request reprint Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo
    Rainer Machauer
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, PO Box, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 19:1366-70. 2009
  8. ncbi request reprint Conformationally constrained mimics of the membrane-proximal domain of Fc epsilonRIalpha
    Carsten Peters
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, 1235 Vienna, Austria
    Chembiochem 8:1785-9. 2007
  9. ncbi request reprint Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE)
    Stephen Hanessian
    Department of Chemistry, Universite de Montreal, C P 6128, Station Centre Ville, Montreal, Quebec H3C 3J7, Canada
    J Med Chem 49:4544-67. 2006
  10. ncbi request reprint Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics
    Stephen Hanessian
    Department of Chemistry, Universite de Montreal, C P 6128, Succursale Centre Ville, Montreal, Province Quebec, Canada H3C 3J7
    J Med Chem 48:5175-90. 2005

Collaborators

Detail Information

Publications10

  1. ncbi request reprint Structure-based design and protein X-ray analysis of a protein kinase inhibitor
    Pascal Furet
    Novartis Pharmaceuticals Inc, Oncology Research, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 12:221-4. 2002
    ..In addition, it revealed an alternative binding orientation involving a second tautomeric form of the inhibitor that was not envisaged during the design stage...
  2. 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...
  3. doi 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...
  4. doi request reprint Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application
    Andreas Lerchner
    Novartis Institutes for BioMedicalResearch, Novartis Pharma AG, PO Box, CH 4002, Basel, Switzerland
    Bioorg Med Chem Lett 20:603-7. 2010
    ..Several compounds from this series demonstrated acute reduction of Abeta in human APP-wildtype transgenic (APP51/16) mice after oral administration...
  5. doi request reprint Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors
    Rainer Machauer
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, PO Box, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 19:1361-5. 2009
    ..These inhibitors show improved enzymatic potency over their open-chain analogue. Inhibitor 3h also shows activity in a cellular system...
  6. doi request reprint Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors
    Heinrich Rueeger
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, PO Box, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 21:1942-7. 2011
    ..Inhibitors of sub-micromolar potency with an improved property profile over historic HEA inhibitors resulting in improved brain penetration are described...
  7. doi request reprint Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo
    Rainer Machauer
    Novartis Institutes for BioMedical Research, Novartis Pharma AG, PO Box, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 19:1366-70. 2009
    ..Variation of the P' moiety resulted in the macrocyclic inhibitor 14. Both macrocycles show inhibition of BACE-1 in the brain of APP51/16 transgenic mice, 3 (NB-544) after intravenous and 14 (NB-533) after oral application...
  8. ncbi request reprint Conformationally constrained mimics of the membrane-proximal domain of Fc epsilonRIalpha
    Carsten Peters
    Novartis Institutes for BioMedical Research, Brunner Strasse 59, 1235 Vienna, Austria
    Chembiochem 8:1785-9. 2007
  9. ncbi request reprint Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE)
    Stephen Hanessian
    Department of Chemistry, Universite de Montreal, C P 6128, Station Centre Ville, Montreal, Quebec H3C 3J7, Canada
    J Med Chem 49:4544-67. 2006
    ..Cocrystal structures of two synthetic analogues revealed interesting and unexpected binding interactions...
  10. ncbi request reprint Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics
    Stephen Hanessian
    Department of Chemistry, Universite de Montreal, C P 6128, Succursale Centre Ville, Montreal, Province Quebec, Canada H3C 3J7
    J Med Chem 48:5175-90. 2005
    ..X-ray cocrystal structures of two analogues 5 and 45 revealed excellent convergence with the original inhibitor 1 structure while providing new insights into other interactions which could be exploited for future modifications...