Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375154 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
A panel of amino acid analogs and conformationally-restricted amino acids bearing a sulfonic acid were synthesized and tested for their ability to preferentially inhibit the obligate cysteine–glutamate transporter system xc- versus the vesicular glutamate transporter (VGLUT). Several promising candidate molecules were identified: R/S -4-[4′-carboxyphenyl]-phenylglycine, a biphenyl substituted analog of 4-carboxyphenylglycine and 2-thiopheneglycine-5-sulfonic acid both of which reduced glutamate uptake at system xc- by 70–75% while having modest to no effect on glutamate uptake at VGLUT.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jean-Louis G. Etoga, S. Kaleem Ahmed, Sarjubhai Patel, Richard J. Bridges, Charles M. Thompson,