Description of Research Program
Our research addresses the development and exploitation of novel strategies of rational drug design, with a focus on peptide-based therapeutics.  We have demonstrated dramatic improvements in the activities, stabilities, selectivities, and barrier-crossing efficiencies of peptide therapeutic candidates utilizing our strategies, which have been patented.  Therapeutic candidates under current development include antithrombotic, antipsychotic, and antiviral peptides; our strategies can be applied to virtually any peptide of therapeutic interest.  We also are developing biochemical tools such as receptor-specific peptide analogs, which then will be used to define the detailed physiological roles of individual members of receptor families.

Selected Publications
K. P. Kokko; M.K. Hadden, and T. A. Dix* (2002) “Quantification of Neurotensin[8-13] Degradation in Human and Rat Serum Utilizing Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Mass Spectrometry” Anal. Biochem., 308, 34-41.

K. J. Kennedy, Kevin S. Orwig, J. Christopher, A. A. Jaffa, and T. A. Dix* (2002) “Synthesis and Analysis of Potent, More Lipophilic Derivatives of the Bradykinin B2 Receptor Antagonist Peptide HOE 140.” J. Peptide Res., 59, 139-148.

J. T. Lundquist, IV, E. E. Büllesbach; P. Golden, and T. A. Dix* (2002) “Topography of the Neurotensin(NT)(8-9) Binding Site of Human NT receptor-1 Probed with NT(8-13) Analogues.” J. Peptide Res. 59, 55-61.

K. P. Kokko, C. E. Arrigoni and T. A. Dix* (2001)“Selectivity Enhancement Induced by Substitution of Non-natural Analogs of Arginine and Lysine in Arginine-based Thrombin Inhibitors” Bioorg. Med. Chem. Letts., 11, 1947-1950.

K. J. Kennedy, J. T. Lundquist, IV, T. L. Simandan, K. P. Kokko, C. C. Beeson and T. A. Dix* “Design Rationale, Synthesis, and Characterization of Non-Natural Analogues of the Cationic Amino Acids Arginine and Lysine.” (2000) J. Peptide Res. 55, 348-358.

J. T. Lundquist, IV, E. E. Büllesbach, and T. A. Dix* “Synthesis of Neurotensin(9–13) Analogues Exhibiting Enhanced Human Neurotensin Receptor Binding Affinities.” Bioorg. Med. Chem. Letts. (2000) 10, 453-455.