ArticleACS central science2023
Kinase-Modulated Bioluminescent Indicators Enable Noninvasive Imaging of Drug Activity in the Brain.
Article in ACS central science, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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
16 citing papers in PubMed, 21 citations in OpenAlex.
- Prime editing in neuropsychiatric disorders: From mutation-specific target selection to clinical translation.Neuroprotection (Chichester, England) · 2026Review
- Fast analysis and engineering of protein function by microbe-independent deep assembly and screening.Molecular systems biology · 2026Article
- Bright calcium-modulated bioluminescent indicators for activity imaging and red photon-assisted synaptic transmission.bioRxiv : the preprint server for biology · 2026Article
- Pharmacodynamics of Akt drugs revealed by a kinase-modulated bioluminescent indicator.Nature chemical biology · 2025Article
- Visualizing drug effects over time in live animals using optical pharmacodynamics.Nature chemical biology · 2025Article
- Luciferase complementation for cellular assays beyond protein-protein interactions.Analytical sciences : the international journal of the Japan Society for Analytical Chemistry · 2025Review
- MEK Inhibition Enhances the Antitumor Effect of Radiotherapy in NF1-Deficient Glioblastoma.Molecular cancer therapeutics · 2024Article
- Emerging Synthetic Bioluminescent Reactions for Non-Invasive Imaging of Freely Moving Animals.International journal of molecular sciences · 2024Review
- Next-Generation Genetically Encoded Fluorescent Biosensors Illuminate Cell Signaling and Metabolism.Annual review of biophysics · 2024Review
- Review
- Recent advances in bioluminescent probes for neurobiology.Neurophotonics · 2024Article
- Leveraging yeast sequestration to study and engineer posttranslational modification enzymes.Biotechnology and bioengineering · 2024Review
- Intracellular Protein Delivery: Approaches, Challenges, and Clinical Applications.BME frontiers · 2024Review
- Chemical Sensors and Imaging: Molecular, Materials, and Biological Platforms.ACS central science · 2023Article
- Engineered Bioluminescent Indicator Enables the Brain Imaging of Kinase Inhibitors.ACS central science · 2023Article
- Successes and challenges in modeling heterogeneous BRAFFrontiers in oncology · 2023Review
Corrections and comments
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Authors and funding
8 authors at 4 institutions in 2 countries.
Funding
Abstract
Aberrant kinase activity contributes to the pathogenesis of brain cancers, neurodegeneration, and neuropsychiatric diseases, but identifying kinase inhibitors that function in the brain is challenging. Drug levels in blood do not predict efficacy in the brain because the blood-brain barrier prevents entry of most compounds. Rather, assessing kinase inhibition in the brain requires tissue dissection and biochemical analysis, a time-consuming and resource-intensive process. Here, we report kinase-modulated bioluminescent indicators (KiMBIs) for noninvasive longitudinal imaging of drug activity in the brain based on a recently optimized luciferase-luciferin system. We develop an ERK KiMBI to report inhibitors of the Ras-Raf-MEK-ERK pathway, for which no bioluminescent indicators previously existed. ERK KiMBI discriminates between brain-penetrant and nonpenetrant MEK inhibitors, reveals blood-tumor barrier leakiness in xenograft models, and reports MEK inhibitor pharmacodynamics in native brain tissues and intracranial xenografts. Finally, we use ERK KiMBI to screen ERK inhibitors for brain efficacy, identifying temuterkib as a promising brain-active ERK inhibitor, a result not predicted from chemical characteristics alone. Thus, KiMBIs enable the rapid identification and pharmacodynamic characterization of kinase inhibitors suitable for treating brain diseases.
Identifiers
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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.