Publications by authors named "Corinne R Ley"
Article Synopsis
- A new generation of tunable pH-sensitive linkers based on phosphoramidate has been developed to release drugs specifically in acidic conditions without needing enzymes.
- The design focuses on optimizing features like amine type, stability in biological settings, and controlled release rates at different pH levels, particularly in intracellular compartments.
- Innovations, such as using a carboxylic acid nearby, enhance hydrolysis of the linkers for targeted amine release, and protective esterification indicates potential for these linkers to be used as prodrugs for oral administration.
Prostate-specific membrane antigen (PSMA) is a cell-surface enzyme-biomarker that is actively pursued for targeted delivery of imaging and therapeutic agents for prostate cancer. Our lab has developed PSMA inhibitors based on a phosphoramidate scaffold, which has shown both high selectivity for PSMA-positive tumors and rapid clearance in vivo when radiolabeled with (18)F. However, this scaffold exhibits hydrolytic instability under low pH and high temperature conditions, barring the use of other imaging or therapeutic radionuclides such as (68)Ga or (177)Lu.
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