Resume

• 2007

  Dartmouth College

  Dartmouth College

  UCSD

  Doctor of Philosophy (Ph.D.)

  Chemistry

  UCI

  Bachelor of Science (BSc)

• Science

  Structural Biology

  University Teaching

  Higher Education

  Drug Design

  Small Molecule Inhibition of the Na+/H+ Exchange Regulatory Factor 1 and Parathyroid Hormone 1 Receptor Interaction

  We have identified a series of small molecules that bind to the canonical peptide binding grove of the PDZ1 domain of NHERF1 and effectively compete with the association of the C-terminus of parathyroid hormone 1 receptor (PTH1R). Employing NMR and molecular modeling we characterize the mode of binding which involves the GYGF loop important for the association of the C-terminus of PTH1R. We demonstrate that the common core of the small molecules binds to the PDZ1 domain of NHERF1 and displaces an 15N-labeled peptide corresponding to the C-terminus of PTH1R. The small size (molecular weight of 192) of this core scaffold makes it an excellent candidate for further elaboration in the development of an inhibitor for this important protein-protein interaction.

  Small Molecule Inhibition of the Na+/H+ Exchange Regulatory Factor 1 and Parathyroid Hormone 1 Receptor Interaction

  Dale