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References from Systematic PEGylation optimization of Dar3A-based FAP-targeted PET probes and first-in-human study. Local targets link to admitted publications; unresolved targets remain external evidence.
Radioactive transition metals for imaging and therapy
10.1021/acs.chemrev.8b00281 · 2019 · External reference
Radioactive main group and rare earth metals for imaging and therapy
10.1021/acs.chemrev.8b00294 · 2019 · External reference
Medicinal inorganic chemistry - challenges, opportunities and guidelines to develop the next generation of radioactive, photoactivated and active site inhibiting metal-based medicines
10.1039/d2cs00407k · 2022 · External reference
Chemical tools to characterize the coordination chemistry of radionuclides for radiopharmaceutical applications
10.1021/acs.chemrev.5c00641 · 2025 · External reference
Radiochemistry for positron emission tomography
10.1038/s41467-023-36377-4 · 2023 · External reference
Matching chelators to radiometals for radiopharmaceuticals
10.1039/c3cs60304k · 2014 · External reference
Emerging chelators for nuclear imaging
10.1016/j.cbpa.2021.03.001 · 2021 · External reference
Design, synthesis, and preclinical evaluation of a novel bifunctional macrocyclic chelator for theranostics of cancers
10.1007/s00259-022-05750-8 · 2022 · External reference
Development of Dar3A chelator and construction of FAP-targeted PET probe as proof of concept and for first-in-human evaluation
10.2967/jnumed.125.271421 · 2026 · External reference
Cancer-associated fibroblasts and tumor growth—bystanders turning into key players
10.1016/j.gde.2009.01.003 · 2009 · External reference
Cell surface glycoprotein of reactive stromal fibroblasts as a potential antibody target in human epithelial cancers
10.1073/pnas.87.18.7235 · 1990 · External reference
FAPI PET/CT: will it end the hegemony of (18)F-FDG in oncology?
10.2967/jnumed.120.256271 · 2021 · External reference
Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP)
10.1021/jm500031w · 2014 · External reference
Development of quinoline-based theranostic ligands for the targeting of fibroblast activation protein
10.2967/jnumed.118.210443 · 2018 · External reference
Development of fibroblast activation protein-targeted radiotracers with improved tumor retention
10.2967/jnumed.118.224469 · 2019 · External reference
Fibroblast activation protein targeting probe with Gly-pro sequence for PET of glioblastoma
10.1021/acs.molpharmaceut.3c00248 · 2023 · External reference
Structure-property investigation of new “KetoFAPI” inhibitors of fibroblast activation protein (FAP): discovery of highly potent, selective compounds with prolonged residence times and promising radiotheranostic potential
10.1021/acs.jmedchem.5c02102 · 2025 · External reference
Covalent targeted radioligands potentiate radionuclide therapy
10.1038/s41586-024-07461-6 · 2024 · External reference
Chelator-guided radiosynthesis, preclinical evaluation, and clinical study of [(68)Ga]Ga-TRAP-(FAPI)(3) for positron emission tomography imaging of tumors
10.1016/j.jconrel.2026.114908 · 2026 · External reference
Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy
10.1007/s00259-022-05842-5 · 2022 · External reference
Small molecule-drug conjugates: an emerging drug design strategy for targeted therapeutics
10.1021/acs.jmedchem.5c01861 · 2025 · External reference
Modification of asp-peptide adapters: giving the FAP-targeted radioligand a “squirrel tail”
10.1021/acs.jmedchem.4c03133 · 2025 · External reference
Noninvasive imaging of FAP expression using positron emission tomography: a comparative evaluation of a [(18)F]-labeled glycopeptide-containing FAPI with [(18)F]FAPI-42
10.1007/s00259-023-06282-5 · 2023 · External reference
Structure-guided designed [(18)F]-labeled FAPI for enhanced hydrophilicity: from preclinical to first-in-human study
10.1021/acs.jmedchem.5c03486 · 2026 · External reference
Design, synthesis, and evaluation of a novel positron emission tomography tracer targeting fibroblast activation protein: from bench to bedside
10.1021/acs.jmedchem.4c02961 · 2025 · External reference
Effect of pegylation on pharmaceuticals
10.1038/nrd1033 · 2003 · External reference
State of the art in PEGylation: the great versatility achieved after forty years of research
10.1016/j.jconrel.2011.10.037 · 2012 · External reference
PEG spacers of different length influence the biological profile of bombesin-based radiolabeled antagonists
10.1016/j.nucmedbio.2014.03.014 · 2014 · External reference
Synthesis and in vivo and in vitro properties of (99m)Tc-labeled fibroblast activation protein inhibitors
10.1021/acs.molpharmaceut.5c01874 · 2026 · External reference
Poly(ethylene glycol) in drug delivery: pros and cons as well as potential alternatives
10.1002/anie.200902672 · 2010 · External reference
Drug-target residence time and its implications for lead optimization
10.1038/nrd2082 · 2006 · External reference
Docking and scoring in virtual screening for drug discovery: methods and applications
10.1038/nrd1549 · 2004 · External reference
Drug-target residence time affects in vivo target occupancy through multiple pathways
10.1021/acscentsci.9b00770 · 2019 · External reference
A modeling analysis of the effects of molecular size and binding affinity on tumor targeting
10.1158/1535-7163.mct-09-0195 · 2009 · External reference
Delivery of molecular and nanoscale medicine to tumors: transport barriers and strategies
10.1146/annurev-chembioeng-061010-114300 · 2011 · External reference
FAP radioligand linker optimization improves tumor dose and tumor-to-healthy organ ratios in 4T1 syngeneic model
10.1021/acs.jmedchem.4c00448 · 2024 · External reference
Precise PEGylation modulates the in vivo fate of peptide radiopharmaceuticals
10.1002/smll.202410410 · 2025 · External reference
FAPI dimerization for theranostic applications: molecular design, preclinical validation, and clinical translation
10.1021/cbmi.6c00005 · 2026 · External reference
Do enthalpy and entropy distinguish first in class from best in class?
10.1016/j.drudis.2008.07.005 · 2008 · External reference
Depletion of stromal cells expressing fibroblast activation protein-α from skeletal muscle and bone marrow results in cachexia and anemia
10.1084/jem.20122344 · 2013 · External reference