Structural determinants of substrates and inhibitors: probing glutamate transporters with 2, 4-methanopyrroldidine-2, 4-dicarboxylate

…, MP Kavanaugh, DP Philips, AR Chamberlin…

Index: Esslinger, C. Sean; Koch, Hans P.; Kavanaugh, Michael P.; Philips, Dean P.; Chamberlin, A. Richard; Thompson, Charles M.; Bridges, Richard J. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 21 p. 3101 - 3106

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Citation Number: 37

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 non-substrate inhibitors of a high-affinity, sodium- dependent glutamate transporter.