Characterizing unexpected interactions of a glutamine transporter inhibitor with members of the SLC1A transporter family.

ABSTRACT: The solute carrier 1A family comprises a group of membrane proteins that act as dual-function amino acid transporters and chloride (Cl^-) channels and includes the alanine serine cysteine transporters (ASCTs) as well as the excitatory amino acid transporters. ASCT2 is regarded as a promising target for cancer therapy, as it can transport glutamine and other neutral amino acids into cells and is upregulated in a range of solid tumors. The compound L-γ-glutamyl-p-nitroanilide (GPNA) is widely used in studies probing the role of ASCT2 in cancer biology; however, the mechanism by which GPNA inhibits ASCT2 is not entirely clear. Here, we used electrophysiology and radiolabelled flux assays to demonstrate that GPNA activates the Cl^- conductance of ASCT2 to the same extent as

SUBMITTER: Freidman NJ 

PROVIDER: S-EPMC9293768 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature