Structural determinants of substrates and inhibitors: Probing glutamate transporters with 2,4-methanopyrrolidine-2,4-dicarboxylate

C. Sean Esslinger, Hans P. Koch, Michael P. Kavanaugh, Dean P. Philips, A. Richard Chamberlin, Charles M. Thompson, Richard J. Bridges

Research output: Contribution to journalArticlepeer-review

43 Scopus citations

Abstract

Using an intramolecular [2+2] photocyclization, 2,4-methanopyrrolidine- 2,4-dicarboxylate was prepared as a conformationally locked analogue of glutamate. This compound, in combination with two other pyrrolidine dicarboxylates, has been used to define the structural elements that differentiate substrate and nonsubstrate inhibitors of a high-affinity, sodium-dependent glutamate transporter.

Original languageEnglish
Pages (from-to)3101-3106
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume8
Issue number21
DOIs
StatePublished - Nov 1998

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