Synthesis of novel neutrophil-specific imaging agents for Positron Emission Tomography (PET) imaging
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Acknowledgments
The research was supported by Commonwealth Foundation for Cancer Research (D.P.) NIH Grants HL-073361 (J.L.) and HD051609 (K.D.F.).
References and notes (7)
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2023, Advanced Drug Delivery ReviewsCitation Excerpt :These can be categorised into metabolic radiotracers based on amino acids (e.g. [11C]methionine, L-[3-18F]-α-methyltyrosine, [18F]fluoroethyltyrosine), nucleic acids (e.g. 3′-deoxy-3′-[18F]fluorothymidine, [11C]thymidine), lipids or lipid metabolism (e.g. [11C]acetate, [11C]choline, [18F]fluorocholine), radiotracers that detect hypoxia (e.g. [18F]fluoromisonidazole, [18F]FAZA, [64Cu]Cu-ATSM) or apoptosis (radiolabelled annexin V),[75,76] radiolabelled hormone analogues ([18F]fluoroestradiol for oestrogen receptors, [18F]fluorodihydrotestosterone for androgen receptors, radiolabelled octreotide analogues for somatostatin receptors), radiotracers based on surface proteins overexpressed in tumour cells (e.g. folate receptors, radiolabelled RGD peptides for integrin αVβ3, [18F]fluoroDOPA for brain tumours, 68Ga-labelled fibroblast activation protein (FAP) inhibitors,[77,78] and the tumour micro-environment (e.g. 64Cu-labelled nanoparticles to image tumour-associated macrophages.[79] Numerous PET and SPECT radiotracers have also been developed with the aim of imaging non-malignant lung diseases, for example [64Cu]Cu-PEG-FLFLFK to image neutrophils in lung infections,[80–82] 68Ga-labelled nanoparticles for neutrophils in lung inflammation,[83] 64Cu-labelled integrin αvβ6- targeting peptides for idiopathic pulmonary fibrosis and lung cancer,[84] 99mTc-labelled interleukin 8 for lung infections.[85] Recently, 68Ga- and 18F-labelled FAP inhibitors have shown promising results for the imaging of activated fibroblasts in interstitial lung diseases.[86,87]
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2020, European Journal of RadiologyCitation Excerpt :Neutrophils are thought to be a key driver of the response of the immune system, active in the early stages of the immune response; in-vivo detection of neutrophils would allow early investigation of acute response. The antagonist, cinnamoyl-F-(D)L-F-(D)L-F (cFLFLF), was identified early as a peptide probe which binds with high affinity to the neutrophil N-formylpeptide receptor (FPR) [65]; improved radiochemistry was achieved with the compound cFLFLF-PEG-DOTA labelled with 64Cu [66]. Evaluation of this tracer in a murine model of bacterial inflammation (n = 6) revealed a 5 fold increase in signal in infected lungs compared with control lungs (n = 4) [67].
MUB <inf>40</inf> Binds to Lactoferrin and Stands as a Specific Neutrophil Marker
2018, Cell Chemical BiologyCitation Excerpt :Further investigations will be required to validate RI-MUB40 as a potentially new inflammation marker in vivo, including a preclinical study (toxicity, bioavailability, specificity, and sensitivity of its lactoferrin-binding property). Labeling RI-MUB40 with radioactive elements may be envisaged for inflammation site localization with non-invasive inflammation-imaging methods such as scintigraphy, positron emission tomography, or single-photon emission computed tomography (Wu et al., 2013; Zhang et al., 2010; Zhang et al., 2007; Locke et al., 2009). Neutrophils are major players of the innate immune response during inflammation and infection, although their detection remains difficult in animal models and humans.
PET imaging detection of macrophages with a formyl peptide receptor antagonist
2015, Nuclear Medicine and BiologyCitation Excerpt :In mammals, there are three FPR receptor subtypes, including FPR1, FPR2 and FPR3, which share significant sequence homology and are encoded by three adjacent genes. As FPRs are mainly restricted to leukocytes, the cFLFLF peptide has been used to evaluate inflammation involving neutrophils [12–14]. A recent study has shown that FPR1 is more abundantly expressed by macrophages than neutrophils [11].