Diester Prodrugs of a Phosphonate Butyrophilin Ligand Display Improved Cell Potency, Plasma Stability, and Payload Internalization
Umed Singh,
Girija Pawge,
Sarita Rani
et al.
Abstract:Activation of Vγ9Vδ2
T cells with butyrophilin
3A1
(BTN3A1) agonists such as (
E
)-4-hydroxy-3-methyl-but-2-enyl
diphosphate (HMBPP) has the potential to boost the immune response.
Because HMBPP is highly charged and metabolically unstable, prodrugs
may be needed to overcome these liabilities, but the prodrugs themselves
may be limited by slow payload release or low plasma stability. To
identify effective prodrug forms of a phosphonate agonist of BTN3A1,
we have prepared a set of diester… Show more
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