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Design and Validation of Fibroblast Activation Protein Alpha Targeted Imaging and Therapeutic Agents by Jyoti Roy; Suraj U Hettiarachchi; Miranda Kaake; Ramesh Mukkamala; Philip S Low is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Design and Validation of Fibroblast Activation Protein Alpha Targeted Imaging and Therapeutic Agents about?

**Background**: Cancer-associated fibroblasts (CAFs) comprise a major cell type in the tumor microenvironment where they support tumor growth and survival by producing extracellular matrix, secreting immunosuppressive cytokines, releasing growth factors, and facilitating metastases. Because tumors with elevated CAFs are characterized by poorer prognosis, considerable effort is focused on developing methods to quantitate, suppress and/or eliminate CAFs. We exploit the elevated expression of fibroblast activation protein (FAP) on CAFs to target imaging and therapeutic agents selectively to these fibroblasts in solid tumors. **Methods**: FAP-targeted optical imaging, radioimaging, and chemotherapeutic agents were synthesized by conjugating FAP ligand (FL) to either a fluorescent dye, technetium-99m, or tubulysin B hydrazide. In vitro and in vivo studies were performed to determine the specificity and selectivity of each conjugate for FAP in vitro and in vivo. **Results**: FAP-targeted imaging and therapeutic conjugates showed high binding specificity and affinity in the low nanomolar range. Injection of FAP-targeted ^99m^Tc into tumor-bearing mice enabled facile detection of tumor xen

Who reads Design and Validation of Fibroblast Activation Protein Alpha Targeted Imaging and Therapeutic Agents?

Author

Jyoti Roy; Suraj U Hettiarachchi; Miranda Kaake; Ramesh Mukkamala; Philip S Low

Published

2020

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)