Rodney L. Johnson, Ph.D. Professor Department of Medicinal Chemistry Office: 8-172 Weaver-Densford Hall Telephone Number: 612-624-7997 FAX Number: 612-624-0139 E-mail Address: johns022@umn.edu

Education:

B.S., University of Minnesota, 1972
Ph.D., University of Kansas, 1976

Research Interests:

Research in my laboratory focuses on the design of peptidomimetics. In this regard, the development of methodology for the synthesis of peptidomimetic scaffolds and conformationally-constrained analogues of amino acids and peptides is a major emphasis.

Peptidomimetics of L-Prolyl-L-leucyl-glycinamide are being synthesized in order to elucidate the bioactive conformation of this peptide and to determine the mechanism by which this peptide modulates the binding of agonists to the dopamine D₂ and D₄ receptors. Peptidomimetics of Smac peptides also are being synthesized in order to develop agents that facilitate anticancer drug-induced apoptosis.

My laboratory is also involved in the synthesis of conformationally constrained analogues of the excitatory amino acid neurotransmitter glutamic acid and the excitatory neurotransmission ligands 2-amino-4-phosphonobutanoic acid and quisqualic acid as potential ligands for the metabotropic glutamic acid receptors.

Publications:

R. L. Johnson, and K. S.S.P. Rao, 2,3-Ethylene- and 2,3-Trimethylene-bridged Analogues of the Group III Metabotropic Glutamate Receptor Ligand 2-Amino-4-phosphonobutanoic Acid. Bioorg. Med. Chem. Lett. 2005, 15, 57-60.

A. P. Vartak, V.G. Young, Jr., and R. L. Johnson, Stereoselective Synthesis of α,α'- Biprolines.  Org. Lett. 2005, 7, 35-38.

R. V. Somu and R. L. Johnson, Synthesis of Pipecolic Acid-Based Spiro Bicyclic Lactam Scaffolds as ß-Turn Mimics. J. Org. Chem. 2005, 70, 5954-5963.

K. Dolbeare, G. F. Pontoriero, S. K. Gupta, R. K. Mishra, R. L. Johnson, Synthesis and Dopamine Receptor Modulating Activity of 3-Substituted gamma-Lactam Peptidomimetics of L-Prolyl-L-leucyl-glycinamide. J. Med. Chem. 2003, 46, 727-733.

M. C. Evans and R. L. Johnson, Triproline Analogues of Pro-Leu-Gly-NH₂ with Pro/Leu and Pro/Phe Chimeric Amino Acids in Position 2. Tetrahedron 2000, 56, 9801-9808.

E. M. Khalil, W. H. Ojala, A. Pradhan, V. D. Nair, W. B. Gleason, R. K. Mishra, and R. L. Johnson. Design, Synthesis, and Dopamine Receptor Modulating Activity of Spiro Bicyclic Peptidomimetrics of L-Prolyl-L-leucyl-glycinamide. J. Med. Chem. 1999, 42, 628-637.

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