ArticleJournal of nuclear medicine : official publication, Society of Nuclear Medicine2012
PET of EGFR expression with an 18F-labeled affibody molecule.
Article in Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
36 citing papers in PubMed, 1 synthesis or guideline pooled it, 61 citations in OpenAlex.
- Current progress and quality of radiomic studies for predicting EGFR mutation in patients with non-small cell lung cancer using PET/CT images: a systematic review.The British journal of radiology · 2021Pooled it
- Ultrasound-Assisted Solid-Phase Affibody Synthesis Using ZPharmaceuticals (Basel, Switzerland) · 2024Article
- A novel dual-labeled small peptide as a multimodal imaging agent for targeting wild-type EGFR in tumors.PloS one · 2022Article
- Multimodal Bone Metastasis-associated Epidermal Growth Factor Receptor Imaging in an Orthotopic Rat Model.Radiology. Imaging cancer · 2021Article
- Novel Receptor Tyrosine Kinase Pathway Inhibitors for Targeted Radionuclide Therapy of Glioblastoma.Pharmaceuticals (Basel, Switzerland) · 2021Review
- PET and SPECT Imaging of the EGFR Family (RTK Class I) in Oncology.International journal of molecular sciences · 2021Review
- The Use of a Non-Conventional Long-Lived Gallium RadioisotopePharmaceutics · 2021Article
- A perspective on the radiopharmaceutical requirements for imaging and therapy of glioblastoma.Theranostics · 2021Review
- Article
- ImmunoPET: Concept, Design, and Applications.Chemical reviews · 2020Review
- Affibody Molecules as Targeting Vectors for PET Imaging.Cancers · 2020Review
- A Comprehensive Review of Non-Covalent Radiofluorination Approaches Using Aluminum [Molecules (Basel, Switzerland) · 2019Review
- The beginning of the end for conventional RECIST - novel therapies require novel imaging approaches.Nature reviews. Clinical oncology · 2019Review
- Affibody-Based PET Imaging to Guide EGFR-Targeted Cancer Therapy in Head and Neck Squamous Cell Cancer Models.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Article
- Automated radiosynthesis of [Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine · 2018Article
- Preclinical Evaluation of [Cells · 2018Article
- Influence of composition of cysteine-containing peptide-based chelators on biodistribution ofAmino acids · 2018Article
- Evaluation of affibody charge modification identified by synthetic consensus design in molecular PET imaging of epidermal growth factor receptor.Molecular systems design & engineering · 2018Article
- Cyclic versus Noncyclic Chelating Scaffold forMolecular pharmaceutics · 2018Article
- Fabrication and evaluation of a γ-PGA-based self-assembly transferrin receptor-targeting anticancer drug carrier.International journal of nanomedicine · 2018Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
unlabelledEpidermal growth factor receptor (EGFR) is often overexpressed in a variety of human cancers, and its expression is associated with poor prognosis for many cancer types. However, an accurate technique to noninvasively image EGFR expression in vivo is not available in the clinical setting. In this research, an Affibody analog, anti-EGFR Ac-Cys-Z(EGFR:1907), was successfully site-specifically (18)F-labeled for PET of EGFR expression.
methodsThe prosthetic group N-[2-(4-(18)F-fluorobenzamido) ethyl] maleimide ((18)F-FBEM) was conjugated to Ac-Cys-Z(EGFR:1907) under mild conditions (pH 7) to produce the probe (18)F-FBEM-Cys-Z(EGFR:1907). The binding affinity and specificity tests of (18)F-FBEM-Cys-Z(EGFR:1907) to EGFR were conducted using A431 cancer cells. Small-animal PET and biodistribution studies were conducted on various mice tumor xenograft models with EGFR overexpression (6 types) after injection of approximately 2.0 MBq of (18)F-FBEM-Cys-Z(EGFR:1907) with or without coinjection of unlabeled Ac-Cys-Z(EGFR:1907) for up to 3 h after injection. A correlation study between (18)F-FBEM-Cys-Z(EGFR:1907) small- animal PET quantification and ex vivo Western blot analysis of tumor EGFR expression was conducted in those 6 types of tumor models.
results(18)F-FBEM-Cys-Z(EGFR:1907) binds to EGFR with low nanomolar affinity (37 nM) in A431 cells. (18)F-FBEM-Cys-Z(EGFR:1907) rapidly accumulated in the tumor and cleared from most of the normal organs except the liver and kidneys at 3 h after injection, allowing excellent tumor-to-normal tissue contrast to be obtained. In the A431 tumor xenograft model, coinjection of the PET probe with 45 μg of Ac-Cys-Z(EGFR:1907) was able to improve the tumor uptake (3.9 vs. 8.1 percentage of the injected radioactive dose per gram of tissue, at 3 h after injection) and tumor imaging contrast, whereas coinjection with 500 μg of Ac-Cys-Z(EGFR:1907) successfully blocked the tumor uptake significantly (8.1 vs. 1.0 percentage of the injected radioactive dose per gram of tissue, at 3 h after injection, 88% inhibition, P < 0.05). Moderate correlation was found between the tumor tracer uptake at 3 h after injection quantified by PET and EGFR expression levels measured by Western blot assay (P = 0.007, R = 0.59).
conclusion(18)F-FBEM-Cys-Z(EGFR:1907) is a novel protein scaffold-based PET probe for imaging EGFR overexpression of tumors, and its ability to differentiate tumors with high and low EGFR expression in vivo holds promise for future clinical translation.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.