Development and Characterization of Novel FAP-Targeted Theranostic Pairs: A Bench-to-Bedside Study.

ABSTRACT: Fibroblast activation protein (FAP) is among the most popular targets in nuclear medicine imaging and cancer theranostics. Several small-molecule moieties (FAPI-04, FAPI-46, etc.) are used for developing FAP-targeted theranostic agents. Nonetheless, the circulation time of FAP inhibitors is relatively short, resulting in rapid clearance via kidneys, low tumor uptake, and associated unsatisfactory treatment efficacy. To address the existing drawbacks, we engineered 3 peptides named FD1, FD2, and FD3 with different circulation times through solid-phase peptide synthesis. All the 3 reported peptides bind to human and murine FAP with single-digit nanomolar affinity measured by surface plasmon resonance. The diagnostic and therapeutic potential of the agents labeled with ⁶⁸Ga and

SUBMITTER: Huang W 

PROVIDER: S-EPMC11066877 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature