Albumin binder–conjugated fibroblast activation protein inhibitor radiopharmaceuticals for cancer therapy

M Xu, P Zhang, J Ding, J Chen, L Huo… - Journal of Nuclear …, 2022 - Soc Nuclear Med
Fibroblast activation protein (FAP) has become an attractive target for diagnosis and
therapy, and a series of FAP inhibitor (FAPI)–based radiotracers has been developed and …

[HTML][HTML] Evans blue-modified radiolabeled fibroblast activation protein inhibitor as long-acting cancer therapeutics

X Wen, P Xu, M Shi, J Liu, X Zeng, Y Zhang, C Shi… - Theranostics, 2022 - ncbi.nlm.nih.gov
Rationale: Fibroblast activation protein (FAP) targeted molecular imaging radiotracers have
shown promising preclinical and clinical results in tumor diagnosis. However, rapid …

[HTML][HTML] Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy

D Zboralski, A Hoehne, A Bredenbeck… - European journal of …, 2022 - Springer
Purpose Fibroblast activation protein (FAP) is a membrane-bound protease that has limited
expression in normal adult tissues but is highly expressed in the tumor microenvironment of …

[HTML][HTML] Head-to-head comparison of different classes of FAP radioligands designed to increase tumor residence time: monomer, dimer, albumin binders, and small …

J Millul, L Koepke, GR Haridas, KMJ Sparrer… - European Journal of …, 2023 - Springer
Purpose Fibroblast activation protein-α (FAP)-targeting radioligands have recently
demonstrated high diagnostic potential. However, their therapeutic value is impaired by the …

Development of quinoline-based theranostic ligands for the targeting of fibroblast activation protein

T Lindner, A Loktev, A Altmann, F Giesel… - Journal of Nuclear …, 2018 - Soc Nuclear Med
Fibroblast activation protein (FAP) is overexpressed in cancer-associated fibroblasts and is
involved in a variety of tumor-promoting activities such as matrix remodeling, angiogenesis …

Rational design and pharmacomodulation of protein-binding theranostic radioligands for targeting the fibroblast activation protein

L Meng, J Fang, L Zhao, T Wang, P Yuan… - Journal of Medicinal …, 2022 - ACS Publications
The fibroblast activation protein (FAP), overexpressed on cancer-associated fibroblasts
(CAFs), has become a valuable target for tumor diagnosis and therapy. However, most FAP …

Development of fibroblast activation protein–targeted radiotracers with improved tumor retention

A Loktev, T Lindner, EM Burger, A Altmann… - Journal of Nuclear …, 2019 - Soc Nuclear Med
Cancer-associated fibroblasts constitute a vital subpopulation of the tumor stroma and are
present in more than 90% of epithelial carcinomas. The overexpression of the serine …

18F- or 177Lu-labeled bivalent ligand of fibroblast activation protein with high tumor uptake and retention

H Li, S Ye, L Li, J Zhong, Q Yan, Y Zhong… - European Journal of …, 2022 - Springer
Purpose Fibroblast activation protein (FAP) has become a promising cancer-related target
for diagnosis and therapy. The aim of this study was to develop a bivalent FAP ligand for …

Fatty acid-conjugated radiopharmaceuticals for fibroblast activation protein-targeted radiotherapy

P Zhang, M Xu, J Ding, J Chen, T Zhang, L Huo… - European Journal of …, 2022 - Springer
Introduction Radiopharmaceuticals that target cancer-associated fibroblasts (CAFs) have
become an increasingly attractive strategy for cancer theranostics. Recently, a series of …

[HTML][HTML] Novel generation of FAP inhibitor-based homodimers for Improved Application in Radiotheranostics

M Martin, S Ballal, MP Yadav, C Bal, Y Van Rymenant… - Cancers, 2023 - mdpi.com
Simple Summary Radiopharmaceuticals targeting the fibroblast activation protein alpha
(FAP) can be used in many different cancer types since FAP is highly expressed in the tumor …