2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transport.

@article{Schulte20162Amino4bisaryloxybenzylaminobutano,
  title={2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transport.},
  author={Michael L. Schulte and Alexandra B Khodadadi and Madison L Cuthbertson and Jarrod A Smith and H Charles Manning},
  journal={Bioorganic & medicinal chemistry letters},
  year={2016},
  volume={26 3},
  pages={1044-1047}
}
Herein, we report the discovery of 2-amino-4-bis(aryloxybenzyl)aminobutanoic acids as novel inhibitors of ASCT2(SLC1A5)-mediated glutamine accumulation in mammalian cells. Focused library development led to two novel ASCT2 inhibitors that exhibit significantly improved potency compared with prior art in C6 (rat) and HEK293 (human) cells. The potency of leads reported here represents a 40-fold improvement over our most potent, previously reported inhibitor and represents, to our knowledge, the… CONTINUE READING
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