ArticleNature chemical biology2017
Quantitating drug-target engagement in single cells in vitro and in vivo.
Article in Nature chemical biology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 52 papers.
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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
52 citing papers in PubMed.
- A 5-Azetidinyl BODIPY-Olaparib Conjugate for PARP-Targeted Nuclear and Orthotopic Oral Tumor Imaging.ChemMedChem · 2026Article
- Development of NanoBRET cellular target engagement assays in primary neurons for activating mutants of p21-activated kinase 1.bioRxiv : the preprint server for biology · 2026Article
- Spatial pharmacology of anti-cancer immunomodulators: a comprehensive review.Frontiers in pharmacology · 2026Review
- Fluorescent PSMA-Targeted Radiotheranostic Compounds for Multiscale Imaging.Bioconjugate chemistry · 2025Article
- Dynamic Tracking ofMolecular pharmaceutics · 2025Article
- PARP trapping is governed by the PARP inhibitor dissociation rate constant.Cell chemical biology · 2024Article
- Quantification of Binding of Small Molecules to Native Proteins Overexpressed in Living Cells.Journal of the American Chemical Society · 2024Article
- Article
- Polyethylene Glycol 3350 (PEG 3350) as a Practical Vehicle for Rapid Reconstitution of PARPi-FL Formulations for Clinical Use.Molecular imaging and biology · 2023Article
- Genetically Encoded Detection of Biosynthetic Protease Inhibitors.ACS synthetic biology · 2023Article
- Monitoring drug-target interactions through target engagement-mediated amplification on arrays and in situ.Nucleic acids research · 2022Article
- A novel strigolactone receptor antagonist provides insights into the structural inhibition, conditioning, and germination of the crop parasite Striga.The Journal of biological chemistry · 2022Article
- Examining the Feasibility of Quantifying Receptor Availability Using Cross-Modality Paired-Agent Imaging.Molecular imaging and biology · 2022Article
- TRIPODD: a Novel Fluorescence Imaging Platform for In Situ Quantification of Drug Distribution and Therapeutic Response.Molecular imaging and biology · 2021Article
- A phase I study of a PARP1-targeted topical fluorophore for the detection of oral cancer.European journal of nuclear medicine and molecular imaging · 2021Article
- PARP1: A Potential Molecular Marker to Identify Cancer During Colposcopy Procedures.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021Article
- SMALL MOLECULE IMAGING AGENT FOR MUTANT KRAS G12C.Advanced therapeutics · 2021Article
- Progress toward B-Cell Lymphoma 6 BTB Domain Inhibitors for the Treatment of Diffuse Large B-Cell Lymphoma and Beyond.Journal of medicinal chemistry · 2021Article
- Quantification of Cellular Drug Biodistribution Addresses Challenges in EvaluatingAdvanced therapeutics · 2021Article
- Label-Free Multimodal Multiphoton Intravital Imaging.Advances in experimental medicine and biology · 2021Article
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8 authors.
Funding
Abstract
Quantitation of drug target engagement in single cells has proven to be difficult, often leaving unanswered questions in the drug development process. We found that intracellular target engagement of unlabeled new therapeutics can be quantitated using polarized microscopy combined with competitive binding of matched fluorescent companion imaging probes. We quantitated the dynamics of target engagement of covalent BTK inhibitors, as well as reversible PARP inhibitors, in populations of single cells using a single companion imaging probe for each target. We then determined average in vivo tumor concentrations and found marked population heterogeneity following systemic delivery, revealing single cells with low target occupancy at high average target engagement in vivo.
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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.