Ligand Discovery for the Alanine-Serine-Cysteine Transporter (ASCT2, SLC1A5) from Homology Modeling and Virtual Screening
Fig 5
Electrophysiological methods confirm predicted activators and inhibitors.
(A-C) Representative whole-cell current traces in response to 1 mM of alanine, L-DOPS, and aminooxetane-3-carboxylate (AOC) applied at the time indicated by the gray bar. (D) Dose response curves for AOC and penicillamine (membrane potential = 0 mV, internal buffer contained 130 mM NaSCN and 10 mM alanine, external buffer contained 140 mM NaCl). (E) Maximum whole-cell currents relative to that induced by 1 mM alanine (membrane potential = 0 mV, internal buffer contained 130 mM NaSCN and 10 mM alanine, external buffer contained 140 mM NaCl).