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Sean Esslinger
Research Associate Professor

Phone:(406) 243-4713

Email: christopher.esslinger@umontana.edu

After completing undergraduate work in Chemistry at New Mexico State University, he received a Ph.D. in Chemistry from Colorado State University in 1992. Following a postdoctoral position at the University of California at Irvine, he moved to the University of Montana in 1995, and became the first NIH postdoctoral fellow in the history of the University of Montana in 1997. In 2000, Dr. Esslinger became one of the initial investigators of the NIH Center for Biomedical Research Excellence in Structural and Functional Neuroscience at The University of Montana. He is a research assistant professor in the Department of Biomedical and Pharmaceutical Sciences, and is affiliated with the Department of Chemistry.

RESEARCH STATEMENT

RESEARCH INTERESTS OF THE ESSLINGER LABORATORY GROUP

Research in the group focuses primarily on the neurochemistry of the amino acid glutamate, the major excitatory signaling molecule in central nervous system (CNS), and the glutamate metabolic precursor glutamine. The overall goal of the research is to delineate the process of membrane translocation within neurons and glia by these amino acids, and how these processes contribute to both normal and diseased brain function. The studies of the ligand / protein interactions occur at the molecular and atomic levels. Through the use of asymmmetric syntheses of amino acid analogues with subsequent molecular modeling of the bioassay data, these interactions are analyzed to determine the important and possibly selective interactions occurring between the ligand and the various transport proteins. Thus, the majority of the work performed in the Esslinger laboratory is the asymmetric syntheses of these amino acid analogues. Testing of these novel synthetic analogues occurs in the Esslinger laboratory as well as the Bridges and Thompson laboratories.

KEY PUBLICATIONS

SELECTED PUBLICATIONS

Mavencamp T.L., Rhoderick J.F., Bridges R.J., Esslinger C.S. “Stereoselective synthesis and preliminary pharmacological evaluation of novel derivatives of L-b-threo-benzyl aspartate as inhibitors of the neuronal glutamate transporter EAAT-3” Bioorg Med Chem (Submitted) (2008).

Gajewski M., Seaver B., Esslinger C.S. “Design, Synthesis, and Biological Activity of Novel Triazole Amino Acids Used to Probe Binding Interactions between Ligand and Neutral Amino Acid Transport Protein SN1" Bioorg. Med Chem. Let. (2007), 17, (15), 4163-4166.

Esslinger C.S., Agarwal S., Gerdes J., Wilson P.A., Davis E.S., Awes A.N., O'Brien E., Mavencamp T., Koch H.P., Poulsen D.J., Rhoderick J.F., Chamberlin A.R., Kavanaugh M.P., and Bridges R.J. “The Substituted Aspartate Analogue L-β-threo-Benzyl-Aspartate Preferentially Inhibits the Neuronal Excitatory Amino Acid Transporter EAAT3.” Neuropharm. (2005), 850-861.

Esslinger C.S., Cybulski K.A., Rhoderick F.J.  “Ny -Aryl Glutamine Analogues as Probes of the ASCT2 Neutral Amino Acid Transporter Binding Site” Bioorg Med Chem  (2005) 13(4): 1111-18.

Bridges R.J., and Esslinger C.S. “The Excitatory Amino Acid Transporters:  Pharmacological Insights on Substrate and Inhibitor Specificity of the EAAT Subtypes”, Pharmacol. & Therap. (2005), 107, (3), 271-285.

Carrigan C.N., Bartlett R.D., Esslinger C.S., Cybulski K.A., Tongcharoensirikul P.,  Bridges R.J., and Thompson C.M.  “Synthesis and in Vitro Pharmacology of Substituted Quinoline-2,4-dicarboxylic Acids as Inhibitors of Vesicular Glutamate Transport” J. Med. Chem. (2002), 45, 2260-2276.

Esslinger C.S., Titus J., Koch H.P., Bridges R.J., Chamberlin A.R. (2002). “Methylation of L-trans-2,4-pyrrolidine dicarboxylate converts the glutamate transport inhibitor from a substrate to a non-substrate inhibitor.” Bioorg Med Chem 2002 10(11): 3509-15.

Carrigan C.N., Esslinger C.S., Bartlett R.D., Bridges R.J., and Thompson C.M. (1999) Quinoline-2,4-dicarboxylic acids: synthesis and evaluation as inhibitors of the glutamate vesicular transporter. Bioorganic & Medicinal Chemistry Letters 9: 2607-2612.

Koch H.P., Kavanaugh M.P., Esslinger C.S., Zerangue N., Humphrey J.M., Amara S.G., Chamberlin A.R., and Bridges R.J. (1999) Differentiation of substrate and nonsubstrate inhibitors of the high-affinity, sodium-dependent glutamate transporters. Molecular Pharmacology 56: 1095-1104.

Esslinger C.S., Koch H.P., Kavanaugh M.P., Philips D.P., Chamberlin A.R., Thompson C.M., Bridges R.J. (1998) Structural Determinants of Substrates and Inhibitors: Probing Glutamate Transporters with Meso-2,4-Methano-2,4-Pyrrolidine Dicarboxylate Bioorganic and Medicinal Chemistry Letters 8: 3101.

Bartlett R.D., Esslinger C.S., Thompson C.M., Bridges R.J.  "Kynurenate Analogues as Inhibitors of L-Glutamate Transport into Synaptic Vesicles" J. Neuropharm. (1998), 37, 839.