ArticleScientific reports2014
Single cell imaging of Bruton's tyrosine kinase using an irreversible inhibitor.
Article in Scientific reports, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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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
20 citing papers in PubMed.
- Visualization of a Bruton's Tyrosine Kinase Inhibitor Using Fluorescence and Raman Microscopy.Analytical chemistry · 2026Article
- Hepatitis B virus reactivation in patients with hematologic malignancies treated with Bruton tyrosine kinase inhibitors.Blood research · 2025Article
- Investigation of Proteome-Tetrazine Reactivity for a Highly Selective Tetrazine Ligation in Live Cells.ACS central science · 2025Article
- Design Principles and Applications of Fluorescent Kinase Inhibitors for Simultaneous Cancer Bioimaging and Therapy.Cancers · 2024Review
- Tumor-Cell-Specific Targeting of Ibrutinib: Introducing Electrostatic Antibody-Inhibitor Conjugates (AiCs).Angewandte Chemie (International ed. in English) · 2022Article
- Fluorescent kinase inhibitors as probes in cancer.Chemical Society reviews · 2021Review
- A Cleavable CJournal of the American Chemical Society · 2020Article
- Understanding the in vivo Fate of Advanced Materials by Imaging.Advanced functional materials · 2020Article
- Single-Cell Intravital Microscopy of Trastuzumab Quantifies Heterogeneous in vivo Kinetics.Cytometry. Part A : the journal of the International Society for Analytical Cytology · 2020Article
- Clinical trials, progression-speed differentiating features and swiftness rule of the innovative targets of first-in-class drugs.Briefings in bioinformatics · 2020Article
- Measurement of drug-target engagement in live cells by two-photon fluorescence anisotropy imaging.Nature protocols · 2017Article
- Imaging the pharmacology of nanomaterials by intravital microscopy: Toward understanding their biological behavior.Advanced drug delivery reviews · 2017Review
- Quantitating drug-target engagement in single cells in vitro and in vivo.Nature chemical biology · 2017Article
- Design and Development of Fluorescent Vemurafenib Analogs forTheranostics · 2017Article
- Fluorescent vinblastine probes for live cell imaging.Chemical communications (Cambridge, England) · 2016Article
- A novel 2,5-diaminopyrimidine-based affinity probe for Bruton's tyrosine kinase.Scientific reports · 2015Article
- Tumour-associated macrophages act as a slow-release reservoir of nano-therapeutic Pt(IV) pro-drug.Nature communications · 2015Article
- Optimized Near-IR Fluorescent Agents for in Vivo Imaging of Btk Expression.Bioconjugate chemistry · 2015Article
- On chip analysis of CNS lymphoma in cerebrospinal fluid.Theranostics · 2015Article
- Fluorescence anisotropy imaging in drug discovery.Advanced drug delivery reviewsReview
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
A number of Bruton's tyrosine kinase (BTK) inhibitors are currently in development, yet it has been difficult to visualize BTK expression and pharmacological inhibition in vivo in real time. We synthesized a fluorescent, irreversible BTK binder based on the drug Ibrutinib and characterized its behavior in cells and in vivo. We show a 200 nM affinity of the imaging agent, high selectivity, and irreversible binding to its target following initial washout, resulting in surprisingly high target-to-background ratios. In vivo, the imaging agent rapidly distributed to BTK expressing tumor cells, but also to BTK-positive tumor-associated host cells.
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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.