2. Academic Validation
  3. Mixed Aryl Phosphonate Prodrugs of a Butyrophilin Ligand

Mixed Aryl Phosphonate Prodrugs of a Butyrophilin Ligand

  • ACS Med Chem Lett. 2017 Aug 9;8(9):914-918. doi: 10.1021/acsmedchemlett.7b00245.
Benjamin J Foust 1,  Michael M Poe 2,  Nicholas A Lentini 1,  Chia-Hung Christine Hsiao 2,  Andrew J Wiemer 2 3,  David F Wiemer 1 4
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Iowa, Iowa City, Iowa 52242-1294, United States.
  • 2 Department of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut 06269-3092 United States.
  • 3 Institute for Systems Genomics, University of Connecticut, Storrs, Connecticut 06269-3092, United States.
  • 4 Department of Pharmacology, University of Iowa, Iowa City, Iowa 52242-1109, United States.
PMID: 28947936 DOI: 10.1021/acsmedchemlett.7b00245
Abstract

Studies of aryl phosphonate derivatives of a butyrophilin 3A1 ligand have resulted in identification of a potent stimulant of Vγ9 Vδ2 T cells. This compound, a mixed ester bearing one pivaloyloxymethyl substituent and one 1-naphthyl ester displayed an EC50 of 0.79 nM as a stimulant of T cell proliferation, and a 9.0 nM EC50 in an assay designed to measure interferon gamma production. In both assays, this is the most potent butyrophilin ligand prodrug yet reported, and thus it should be a valuable tool for studies of T cell function. Furthermore, mixed aryl/acyloxyalkyl esters may represent a new class of phosphonate prodrugs with high efficacy.

Keywords

Aryl phosphonates; BTN3A1; butyrophilin; ligand; phosphoantigen; prodrug.

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