A Trifunctional Theranostic Ligand Targeting Fibroblast Activation Protein-α (FAPα).

James M KellyThomas M JeitnerShashikanth PonnalaClarence WilliamsAnastasia NikolopoulouStephen G DiMagnoJohn W Babich

Published in: Molecular imaging and biology (2021)

RPS-309 is a high-affinity FAPα inhibitor with prolonged plasma residence. Introduction of the albumin-binding group did not compromise FAPα binding. Although initial tumor uptake was high and FAPα-specific, RPS-309 also progressively cleared from tumors. Nevertheless, RPS-309 incorporates multiple sites in which structural diversity can be introduced, and therefore serves as a platform for future structure-activity relationship studies.

Keyphrases

structure activity relationship
binding protein
photodynamic therapy
dna binding
high throughput
cancer therapy
protein protein
fluorescence imaging
transcription factor
case control
drug delivery