Ontology highlight
ABSTRACT:
SUBMITTER: Singh K
PROVIDER: S-EPMC5363072 | biostudies-literature | 2017 Feb
REPOSITORIES: biostudies-literature
Singh Kurnvir K Tanui Rose R Gameiro Armanda A Eisenberg Gilad G Colas Claire C Schlessinger Avner A Grewer Christof C
Bioorganic & medicinal chemistry letters 20161227 3
The glutamine transporter ASCT2 has been identified as a promising target to inhibit rapid growth of cancer cells. However, ASCT2 pharmacology is not well established. In this report, we performed a systematic structure activity analysis of a series of substituted benzylproline derivatives. Substitutions on the phenyl ring resulted in compounds with characteristics of ASCT2 inhibitors. Apparent binding affinity increased with increasing hydrophobicity of the side chain. In contrast, interaction ...[more]