ArticleNuclear medicine and biology
BLZ945 derivatives for PET imaging of colony stimulating factor-1 receptors in the brain.
Article in Nuclear medicine and biology. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 38 citations in OpenAlex.
- Nuclear Medicine Tracers Targeting Tumor-Associated Macrophages.Pharmaceutics · 2026Review
- Evaluation of in vivo and in vitro binding property of a novel candidate PET tracer for CSF1R imaging and comparison with two currently-used CSF1R-PET tracers.EJNMMI radiopharmacy and chemistry · 2025Article
- Evaluation of [Molecular imaging and biology · 2025Article
- PET imaging of neuroinflammation: any credible alternatives to TSPO yet?Molecular psychiatry · 2025Review
- CSF1R antagonism results in increased supraspinal infiltration in EAE.Journal of neuroinflammation · 2024Article
- Fully automated radiosynthesis of [American journal of nuclear medicine and molecular imaging · 2024Article
- Automated radiosynthesis of [American journal of nuclear medicine and molecular imaging · 2024Article
- Candidate Tracers for Imaging Colony-Stimulating Factor 1 Receptor in Neuroinflammation with Positron Emission Tomography: Issues and Progress.ACS pharmacology & translational science · 2023Review
- Synthesis and Evaluation of aPharmaceuticals (Basel, Switzerland) · 2022Article
- Towards PET imaging of the dynamic phenotypes of microglia.Clinical and experimental immunology · 2021Review
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 2 countries.
Funding
Abstract
backgroundThe kinase colony stimulating factor-1 receptor (CSF-1R) has recently been identified as a novel therapeutic target for decreasing tumor associated macrophages and microglia load in cancer treatment. In glioblastoma multiforme (GBM), a high-grade cancer in the brain with extremely poor prognosis, macrophages and microglia can make up to 50% of the total tumor mass. Currently, no non-invasive methods are available for measuring CSF-1R expression in vivo. The aim of this work is to develop a PET tracer for imaging of CSF-1R receptor expression in the brain for future GBM patient selection and treatment monitoring.
methodsBLZ945 and a derivative that potentially allows for fluorine-18 labeling were synthesized and evaluated in vitro to determine their affinity towards CSF-1R. BLZ945 was radiolabeled with carbon-11 by N-methylation of des-methyl-BLZ945 using [
resultsBLZ945 was the most potent compound in our series with an IC
conclusions[
Indexed as
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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.