Potential 18F-labeled biomarkers for epidermal growth factor receptor tyrosine kinase

Bonasera, Thomas A.; Ortu, Giuseppina; Rozen, Yulia; Krais, Roman; Freedman, Nanette; Chisin, Roland; Gazit, Aviv; Levitzki, Alexander; Mishani, Eyal

doi:10.1016/s0969-8051(01)00200-1

Cited by 87 publications

(67 citation statements)

References 19 publications

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“…(15)(16)(17)(18) This study showed that 11 C-PD153035 could be taken up by tumors with different EGFR expression levels. The uptake of tracer 11 C-PD153035, as demonstrated by in vitro accumulation and in vivo biodistribution, closely correlated with the EGFR expression levels of tumor cells.…”

Section: Discussionmentioning

confidence: 70%

Assessment of ¹¹C‐labeled‐4‐N‐(3‐bromoanilino)‐6, 7‐dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression

Wang

Yang

et al. 2007

Cancer Science

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Section: Discussionmentioning

confidence: 70%

Assessment of ¹¹C‐labeled‐4‐N‐(3‐bromoanilino)‐6, 7‐dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression

Wang

Yang

et al. 2007

Cancer Science

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“…3). When 10 6 A431 cells (ϳ2.0 pmol of EGFr) (for B max values see Bonasera et al 15 ) were used (Fig. 3a), 100% inhibition was obtained 2 hr postincubation with 200 pmol of ML03 (50 nM), whereas 8 hr postincubation gave ϳ98% inhibition with the same amount of inhibitor.…”

Section: In Vitro Resultsmentioning

confidence: 97%

“…Measurement of the apparent IC 50 for ML03 was carried out as described by Bonasera et al 15 Briefly, A431 cell lysate was used as the EGFr source. A 96-well ELISA plate was coated with anti-EGFr antibody and the A431 lysate added.…”

Section: Autophosphorylation Inhibition In A431 Cell Lysatementioning

confidence: 99%

“…The amount of protein in each lysate was determined by a filter paper assay described by Bonasera et al 15 The same amount of protein for each sample was then loaded onto an acrylamide gel for a Western blot assay. Blots were incubated with anti-phosphotyrosine, followed by incubation with horseradish peroxidase-conjugated secondary antibody.…”

Section: Autophosphorylation Inhibition Experiments In Whole A431 Cellsmentioning

confidence: 99%

“…In our previous work, 15 we synthesized, labeled and evaluated 4-(fluoroanilino)quinazoline derivatives as EGFrTK PET biomarkers. These molecules bind reversibly to the ATP binding site of the receptor and inhibit the autophosphorylation of the EGFrTK.…”

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Labeled EGFr‐TK irreversible inhibitor (ML03): In vitro and in vivo properties, potential as PET biomarker for cancer and feasibility as anticancer drug

Ortu

Ben-David

Rozen

et al. 2002

Intl Journal of Cancer

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Radiosynthesis of ML03 (N-{4 Key words: carbon-11; cancer; biodistribution; PET; EGFrGrowth factors mediate their pleiotropic actions by binding to and activating receptor tyrosine kinases. Epidermal growth factor receptor (EGFr, erb-B1) belongs to a family of proteins involved in the proliferation of normal and malignant cells. 1,2 The binding of activating ligands such as EGF, TGF ␣, AR, BTC or HB-EGF to the EGFr results in activation of the cytosolic kinase domain. Overexpression of EGFr is the hallmark of many human tumors such as breast cancer, glioma, laryngeal cancer, squamous cell carcinoma of the head and neck and prostate cancer. 3 Since the late 1980s continuous effort has been invested in the development of EGFr tyrosine kinase inhibitors as anti-neoplastic drugs. 4,5-11 Radioactively labeled small molecules with high affinity and selectivity for the tyrosine kinase domain of EGFr might offer a specific and sensitive tool to be used in positron emission tomography (PET) for diagnosis of tumors overexpressing EGFr. PET provides 3D and quantitative maps of the distribution of radioactive tracers within the human body and hence permits the measurement of physiological, biochemical and pharmacological function at the molecular level, both in healthy and pathological states. PET is based on the use of short half-life positron-emitting isotopes, such as 11 C (t 1/2 20.39 min.), 18 F (t 1/2 109.8 min.), 15 O (t 1/2 2.037 min.) and 13 N (t 1/2 9.965 min.). After injection of a suitable biomarker, the PET scan provides a mapping of the biomarker distribution and hence of a specific receptor, transporter or enzyme in the human body. Biomarkers with high selectivity for a specific receptor or enzyme might accumulate in those organs and tissues where the targeted protein is overexpressed. In the case of EGFr, its overexpression in human tumors could be non-invasively detected by labeling tyrosine kinase inhibitors with positron-emitting isotopes. The PET application of these potential biomarkers represents a new strategy for the diagnosis of EGFr-expressing tumors. [12][13][14] Moreover, the increasing demand to incorporate diagnostics into clinical studies of EGFr-targeted therapies suggests a potential future use of EGFrTK labeled inhibitors. These labeled inhibitors could help select patients for clinical trials. Cancer patients could undergo a non-invasive diagnostic PET study with labeled EGFrTK inhibitor, and if their tumor is found to overexpress EGFrTK, they could then be selected for a clinical trial that utilizes anti-EGFr therapy.In our previous work, 15 we synthesized, labeled and evaluated 4-(fluoroanilino)quinazoline derivatives as EGFrTK PET biomarkers. These molecules bind reversibly to the ATP binding site of the receptor and inhibit the autophosphorylation of the EGFrTK. Competition with intracellular ATP results in their fast dissociation from the EGFr kinase site, however, making these compounds ineffective as PET reporter probes. We therefore concluded that irreversible EGFr tyrosine kinase ...

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Design of Turn‐On Near‐Infrared Fluorescent Probes for Highly Sensitive and Selective Monitoring of Biopolymers

et al. 2020

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Simple, sensitive, and selective detection of specific biopolymers is critical in a broad range of biomedical and technological areas. We present a design of turn‐on near‐infrared (NIR) fluorescent probes with intrinsically high signal‐to‐background ratio. The fluorescent signal generation mechanism is based on the aggregation/de‐aggregation of phthalocyanine chromophores controlled by selective binding of small‐molecule “anchor” groups to a specific binding site of a target biopolymer. As a proof‐of‐concept, we demonstrate a design of a sensor for EGFR tyrosine kinase—an important target in cancer research. The universality of the fluorescent signal generation mechanism, as well as the dependence of the response selectivity on the choice of the small‐molecule “anchor” group, make it possible to use this approach to design reliable turn‐on NIR fluorescent sensors for detecting specific protein targets present in the low‐nanomolar concentration range.

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Potential 18F-labeled biomarkers for epidermal growth factor receptor tyrosine kinase

Cited by 87 publications

References 19 publications

Assessment of ¹¹C‐labeled‐4‐N‐(3‐bromoanilino)‐6, 7‐dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression

Assessment of ¹¹C‐labeled‐4‐N‐(3‐bromoanilino)‐6, 7‐dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression

Labeled EGFr‐TK irreversible inhibitor (ML03): In vitro and in vivo properties, potential as PET biomarker for cancer and feasibility as anticancer drug

Design of Turn‐On Near‐Infrared Fluorescent Probes for Highly Sensitive and Selective Monitoring of Biopolymers

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Potential 18F-labeled biomarkers for epidermal growth factor receptor tyrosine kinase

Cited by 87 publications

References 19 publications

Assessment of 11C‐labeled‐4‐N‐(3‐bromoanilino)‐6, 7‐dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression

Assessment of 11C‐labeled‐4‐N‐(3‐bromoanilino)‐6, 7‐dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression

Labeled EGFr‐TK irreversible inhibitor (ML03): In vitro and in vivo properties, potential as PET biomarker for cancer and feasibility as anticancer drug

Design of Turn‐On Near‐Infrared Fluorescent Probes for Highly Sensitive and Selective Monitoring of Biopolymers

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Assessment of ¹¹C‐labeled‐4‐N‐(3‐bromoanilino)‐6, 7‐dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression

Assessment of ¹¹C‐labeled‐4‐N‐(3‐bromoanilino)‐6, 7‐dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression