Journal article
Mixed Aryl Phosphonate Prodrugs of a Butyrophilin Ligand
ACS Medicinal Chemistry Letters, Vol.8(9), pp.914-918
2017
DOI: 10.1021/acsmedchemlett.7b00245
PMCID: PMC5601366
PMID: 28947936
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 EC 50 of 0.79 nM as a stimulant of T cell proliferation, and a 9.0 nM EC 50 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.
Details
- Title: Subtitle
- Mixed Aryl Phosphonate Prodrugs of a Butyrophilin Ligand
- Creators
- Benjamin J Foust - University of IowaMichael M Poe - University of ConnecticutNicholas A Lentini - University of IowaChia-Hung Christine Hsiao - University of ConnecticutAndrew J Wiemer - University of ConnecticutDavid F Wiemer - University of Iowa
- Resource Type
- Journal article
- Publication Details
- ACS Medicinal Chemistry Letters, Vol.8(9), pp.914-918
- DOI
- 10.1021/acsmedchemlett.7b00245
- PMID
- 28947936
- PMCID
- PMC5601366
- NLM abbreviation
- ACS Med Chem Lett
- ISSN
- 1948-5875
- eISSN
- 1948-5875
- Publisher
- American Chemical Society
- Grant note
- DOI: 10.13039/100000057, name: National Institute of General Medical Sciences, award: R01CA186935; DOI: 10.13039/100001024, name: Roy J. Carver Charitable Trust, award: 01-224
- Language
- English
- Date published
- 2017
- Academic Unit
- Neuroscience and Pharmacology; Chemistry
- Record Identifier
- 9983985842402771
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