G Thoma

Summary

Affiliation: Novartis Institutes for BioMedical Research

Publications

  1. ncbi Synthesis and biological evaluation of a potent E-selectin antagonist
    G Thoma
    Novartis Pharma AG, P O Box, CH 4002 Basel, Switzerland, and GlycoTech Corporation, 14915 Broschart Road, Rockville, Maryland 10850, USA
    J Med Chem 42:4909-13. 1999
  2. ncbi Synthesis and biological evaluation of a sialyl Lewis X mimic with significantly improved E-selectin inhibition
    G Thoma
    Novartis Pharma AG, Basel, Switzerland
    Bioorg Med Chem Lett 11:923-5. 2001
  3. ncbi Novel glycodendrimers self-assemble to nanoparticles which function as polyvalent ligands in vitro and in vivo
    Gebhard Thoma
    Novartis Pharma AG, P.O. Box, 4002, Basel, Switzerland
    Angew Chem Int Ed Engl 41:3195-8. 2002
  4. ncbi Orally bioavailable competitive CCR5 antagonists
    Gebhard Thoma
    Novartis Institutes for BioMedical Research, Lichtstrasse 35, WSJ 507 4 12, CH 4056 Basel, Switzerland
    J Med Chem 47:1939-55. 2004
  5. ncbi The chemokine receptor Cxcr3 is not essential for acute cardiac allograft rejection in mice and rats
    H G Zerwes
    Autoimmunity, Transplantation and Inflammation, Novartis Institutes for BioMedical Research, Basel, Switzerland
    Am J Transplant 8:1604-13. 2008
  6. ncbi Removal of anti-Galalpha1,3Gal xenoantibodies with an injectable polymer
    Andreas G Katopodis
    Novartis Institutes for BioMedical Research, Transplantation Research, Basel, Switzerland
    J Clin Invest 110:1869-77. 2002
  7. ncbi Non-covalent polyvalent ligands by self-assembly of small glycodendrimers: a novel concept for the inhibition of polyvalent carbohydrate-protein interactions in vitro and in vivo
    Gebhard Thoma
    Novartis Institutes for BioMedical Research, Lichtstrasse 35, 4056 Basel, Switzerland
    Chemistry 12:99-117. 2005
  8. ncbi Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo
    Gebhard Thoma
    Novartis Institutes for BioMedical Research, Forum 1, Novartis Campus, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 18:2000-5. 2008
  9. ncbi Polymers bearing sLex-mimetics are superior inhibitors of E-selectin-dependent leukocyte rolling in vivo
    Majid Ali
    Cardiovascular Research Group, Clinical Sciences Centre, Northern General Hospital, Sheffield S5 7AU, UK
    FASEB J 18:152-4. 2004

Collaborators

Detail Information

Publications9

  1. ncbi Synthesis and biological evaluation of a potent E-selectin antagonist
    G Thoma
    Novartis Pharma AG, P O Box, CH 4002 Basel, Switzerland, and GlycoTech Corporation, 14915 Broschart Road, Rockville, Maryland 10850, USA
    J Med Chem 42:4909-13. 1999
    ..The assays are predictive for the in vivo efficacy of test compounds as indicated by a marked inhibitory effect of 2 in a thioglycollate induced peritonitis model of acute inflammation in mice (ED(50) approximately 15 mg/kg)...
  2. ncbi Synthesis and biological evaluation of a sialyl Lewis X mimic with significantly improved E-selectin inhibition
    G Thoma
    Novartis Pharma AG, Basel, Switzerland
    Bioorg Med Chem Lett 11:923-5. 2001
    ..Furthermore, compound 5 was highly active (IC50 = 10 microM) in a dynamic non-equilibrium assay in which sLe(x) did not inhibit neutrophil rolling at up to 1000 microM...
  3. ncbi Novel glycodendrimers self-assemble to nanoparticles which function as polyvalent ligands in vitro and in vivo
    Gebhard Thoma
    Novartis Pharma AG, P.O. Box, 4002, Basel, Switzerland
    Angew Chem Int Ed Engl 41:3195-8. 2002
  4. ncbi Orally bioavailable competitive CCR5 antagonists
    Gebhard Thoma
    Novartis Institutes for BioMedical Research, Lichtstrasse 35, WSJ 507 4 12, CH 4056 Basel, Switzerland
    J Med Chem 47:1939-55. 2004
    ..One of these compounds, i.e., 26n, has good PK properties in cynos, and its overall favorable profile makes it a promising candidate for in vivo profiling in transplantation and other disease models...
  5. ncbi The chemokine receptor Cxcr3 is not essential for acute cardiac allograft rejection in mice and rats
    H G Zerwes
    Autoimmunity, Transplantation and Inflammation, Novartis Institutes for BioMedical Research, Basel, Switzerland
    Am J Transplant 8:1604-13. 2008
    ..In summary, Cxcr3 deficiency or pharmacologic blockade does not diminish graft infiltration, tempo and severity of rejection. Thus, Cxcr3 does not appear to play a pivotal role in the allograft rejection models described here...
  6. ncbi Removal of anti-Galalpha1,3Gal xenoantibodies with an injectable polymer
    Andreas G Katopodis
    Novartis Institutes for BioMedical Research, Transplantation Research, Basel, Switzerland
    J Clin Invest 110:1869-77. 2002
    ..Furthermore there was no apparent acute or chronic toxicity associated with GAS914 treatment in primates. We conclude that GAS914 may be used therapeutically for the specific removal of alphaGal Ab's...
  7. ncbi Non-covalent polyvalent ligands by self-assembly of small glycodendrimers: a novel concept for the inhibition of polyvalent carbohydrate-protein interactions in vitro and in vivo
    Gebhard Thoma
    Novartis Institutes for BioMedical Research, Lichtstrasse 35, 4056 Basel, Switzerland
    Chemistry 12:99-117. 2005
    ..The synthesis and characterization of these glycodendrimers is described in detail. Furthermore, we report on the characterization of the non-covalent nanoparticles formed and on their biological evaluation...
  8. ncbi Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo
    Gebhard Thoma
    Novartis Institutes for BioMedical Research, Forum 1, Novartis Campus, CH 4002 Basel, Switzerland
    Bioorg Med Chem Lett 18:2000-5. 2008
    ..Administration of NIBR-1282 in combination with a non-efficacious dose of CsA led to significant prolongation of kidney allograft survival in cynomolgus monkeys...
  9. ncbi Polymers bearing sLex-mimetics are superior inhibitors of E-selectin-dependent leukocyte rolling in vivo
    Majid Ali
    Cardiovascular Research Group, Clinical Sciences Centre, Northern General Hospital, Sheffield S5 7AU, UK
    FASEB J 18:152-4. 2004
    ..In spite of greatly enhanced activity against E-selectin compared with monovalent inhibitor, the multivalent inhibitor had no measurable effect on P- or L-selectin-dependent leukocyte rolling...