B Gay

Summary

Publications

  1. ncbi Effect of potent and selective inhibitors of the Grb2 SH2 domain on cell motility
    B Gay
    Department of Oncology, Novartis Pharma A G, CH 4002 Basel, Switzerland
    J Biol Chem 274:23311-5. 1999
  2. ncbi Selective GRB2 SH2 inhibitors as anti-Ras therapy
    B Gay
    Department of Oncology, Novartis Pharmaceuticals Division, Novartis Ltd, Basel, Switzerland
    Int J Cancer 83:235-41. 1999
  3. ncbi Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain
    P Furet
    Novartis Pharma Inc, Oncology Research Department, CH 4002 Basel, Switzerland
    J Med Chem 41:3442-9. 1998
  4. ncbi Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain
    P Furet
    Novartis Pharma Inc, Oncology Research Department, Basel, Switzerland
    J Med Chem 40:3551-6. 1997
  5. ncbi Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 1
    P Furet
    Novartis Pharmaceuticals, Inc, Therapeutic Area Oncology, Basel, Switzerland
    Bioorg Med Chem Lett 10:2337-41. 2000
  6. ncbi Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic
    P Furet
    Oncology Research Department, Novartis Pharma Inc, CH 4002 Basel, Switzerland
    J Med Chem 42:2358-63. 1999
  7. ncbi Mapping the X(+1) binding site of the Grb2-SH2 domain with alpha,alpha-disubstituted cyclic alpha-amino acids
    C Garcia-Echeverria
    Novartis Pharma Inc, Oncology Research Department, Basel, Switzerland
    Bioorg Med Chem Lett 9:2915-20. 1999
  8. ncbi Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne
    J Schoepfer
    Oncology, Research, Novartis Pharma AG, Basel, Switzerland
    Bioorg Med Chem Lett 11:1201-3. 2001
  9. pmc ErbB-1 and ErbB-2 acquire distinct signaling properties dependent upon their dimerization partner
    M A Olayioye
    Friedrich Miescher Institute, CH 4002 Basel, Switzerland
    Mol Cell Biol 18:5042-51. 1998

Collaborators

Detail Information

Publications9

  1. ncbi Effect of potent and selective inhibitors of the Grb2 SH2 domain on cell motility
    B Gay
    Department of Oncology, Novartis Pharma A G, CH 4002 Basel, Switzerland
    J Biol Chem 274:23311-5. 1999
    ..We demonstrate for the first time a direct role for Grb2 in cell motility and indicate a new avenue for cancer therapeutics...
  2. ncbi Selective GRB2 SH2 inhibitors as anti-Ras therapy
    B Gay
    Department of Oncology, Novartis Pharmaceuticals Division, Novartis Ltd, Basel, Switzerland
    Int J Cancer 83:235-41. 1999
    ..Moreover, our results demonstrate that, in cells overexpressing receptor tyrosine kinases, such as the EGFR, Grb2 SH2 inhibitors induce expression of the cell cycle inhibitors p21(Waf1/Cip1/CAP1) and p27(Kip1) and reverse transformation...
  3. ncbi Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain
    P Furet
    Novartis Pharma Inc, Oncology Research Department, CH 4002 Basel, Switzerland
    J Med Chem 41:3442-9. 1998
    ....
  4. ncbi Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain
    P Furet
    Novartis Pharma Inc, Oncology Research Department, Basel, Switzerland
    J Med Chem 40:3551-6. 1997
    ..The latter confers high affinity (IC50 = 65 nM in an ELISA assay) to the minimal sequence pTyr-Ile-Asn recognized by the Grb2-SH2 domain...
  5. ncbi Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 1
    P Furet
    Novartis Pharmaceuticals, Inc, Therapeutic Area Oncology, Basel, Switzerland
    Bioorg Med Chem Lett 10:2337-41. 2000
    ..The resulting compounds, by exploiting additional interactions, inhibit binding to the Grb2-SH2 domain as potently as the corresponding doubly charged (phosphonomethyl)phenylalanine analogue...
  6. ncbi Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic
    P Furet
    Oncology Research Department, Novartis Pharma Inc, CH 4002 Basel, Switzerland
    J Med Chem 42:2358-63. 1999
    ....
  7. ncbi Mapping the X(+1) binding site of the Grb2-SH2 domain with alpha,alpha-disubstituted cyclic alpha-amino acids
    C Garcia-Echeverria
    Novartis Pharma Inc, Oncology Research Department, Basel, Switzerland
    Bioorg Med Chem Lett 9:2915-20. 1999
    ..The used of alpha,alpha-disubstituted cyclic alpha-amino acids to map the binding pockets of proteins expands the classical alanine scan concept and takes advantage of the known conformational preferences of these amino acids...
  8. ncbi Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne
    J Schoepfer
    Oncology, Research, Novartis Pharma AG, Basel, Switzerland
    Bioorg Med Chem Lett 11:1201-3. 2001
    ..Using Pd(PPh3)2Cl2 as catalyst, selected naphthyl iodides and triflates were coupled to Ac-Pmp(t-Bu)2-Ac6c-Asn-NH(prop-2-ynyl). The resulting alkyne derivatives were hydrogenated and deprotected to afford potent Grb2-SH2 inhibitors...
  9. pmc ErbB-1 and ErbB-2 acquire distinct signaling properties dependent upon their dimerization partner
    M A Olayioye
    Friedrich Miescher Institute, CH 4002 Basel, Switzerland
    Mol Cell Biol 18:5042-51. 1998
    ..Differential receptor phosphorylation may, therefore, be the basis for the differences in the signaling properties observed...