jm015509z_si_001.pdf (929.88 kB)
A Rational Approach to the Design of Selective Substrates and Potent Nontransportable Inhibitors of the Excitatory Amino Acid Transporter EAAC1 (EAAT3). New Glutamate and Aspartate Analogues as Potential Neuroprotective Agents
journal contribution
posted on 2001-07-12, 00:00 authored by Giuseppe Campiani, Meri De Angelis, Silvia Armaroli, Caterina Fattorusso, Bruno Catalanotti, Anna Ramunno, Vito Nacci, Ettore Novellino, Christof Grewer, Diana Ionescu, Thomas Rauen, Roger Griffiths, Colin Sinclair, Elena Fumagalli, Tiziana MenniniTwo three-dimensional receptor interaction models
for EAAT substrates and nontransportable inhibitors have
been developed, and new glutamate (Glu) and aspartate (Asp)
analogues have been synthesized. The analogues 1a and 3
represent novel lead compounds for the development of EAAT
substrates and nontransportable inhibitors, selective for EAATs
over iGluRs, as possible neuroprotective agents useful to
minimize the progression of chronic or acute neurodegenerative diseases. The role played by the protonatable amine
function in the interaction with EAATs has been discussed.