Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 13, Issue 4, Pages 1111-1118Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2004.11.028
Keywords
pharmacophore; modeling; inhibition; H-bonding
Funding
- NCRR NIH HHS [P20 RR15583] Funding Source: Medline
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Analogues of L-glutamine were designed and synthesized to test a hydrogen-bond hypothesis between ligand and neutral amino acid transporter ASCT2. The key design feature contains a substituted phenyl ring on the amide nitrogen that contains electron withdrawing and electron donating groups that alter the pK(a) of the amide NH. Through this study a preliminary binding site map has been developed, and a potent commercially available competitive inhibitor of the ASCT2 transporter has been identified. (C) 2004 Elsevier Ltd. All rights reserved.
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