ArticleJournal of medicinal chemistry2017
A Versatile Method to Determine the Cellular Bioavailability of Small-Molecule Inhibitors.
Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 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
21 citing papers in PubMed, 42 citations in OpenAlex.
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- Blue Fluorescent Siloxytecans Exhibit Potent Anticancer Activity and Enable Direct Real-Time Quantification of Intracellular Uptake.ACS bio & med chem Au · 2026Article
- Optimization of Pyrazolo[3,4‑ACS omega · 2026Article
- Small molecule OPA1 inhibitors amplify cytochrome c release and reverse cancer cells resistance to Bcl-2 inhibitors.Science advances · 2025Article
- Overcoming Challenges in Small-Molecule Drug Bioavailability: A Review of Key Factors and Approaches.International journal of molecular sciences · 2024Review
- Modulation of dynamic DNA G-quadruplex structures in the hTERT promoter region by ligands.Nucleic acids research · 2024Article
- Carbon Dots: A Review with Focus on Sustainability.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Review
- New hemisynthetic derivatives of sphaeropsidin phytotoxins triggering severe endoplasmic reticulum swelling in cancer cells.Scientific reports · 2024Article
- Iterative machine learning-based chemical similarity search to identify novel chemical inhibitors.Journal of cheminformatics · 2023Article
- Investigation of the Effects of Monomeric and Dimeric Stilbenoids on Bacteria-Induced Cytokines and LPS-Induced ROS Formation in Bone Marrow-Derived Dendritic Cells.International journal of molecular sciences · 2023Article
- Structure and inhibition of SARS-CoV-1 and SARS-CoV-2 main proteases by oral antiviral compound AG7404.Antiviral research · 2022Article
- Helical sulfono-γ-AApeptides with predictable functions in protein recognition.RSC chemical biology · 2022Review
- Highly Potent and SelectiveJournal of medicinal chemistry · 2020Article
- Design, Optimization, and Study of Small Molecules That Target Tau Pre-mRNA and Affect Splicing.Journal of the American Chemical Society · 2020Article
- Small-Molecule Inhibition of UBE2T/FANCL-Mediated Ubiquitylation in the Fanconi Anemia Pathway.ACS chemical biology · 2019Article
- Inhibition of β-catenin/B cell lymphoma 9 protein-protein interaction using α-helix-mimicking sulfono-γ-AApeptide inhibitors.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Optimization of Peptidomimetics as Selective Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction.Journal of medicinal chemistry · 2019Article
- A widely-applicable high-throughput cellular thermal shift assay (CETSA) using split Nano Luciferase.Scientific reports · 2018Article
- Structure-Based Optimization of Small-Molecule Inhibitors for the β-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction.Journal of medicinal chemistry · 2018Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
Abstract
The determination of the cellular bioavailability of small-molecule inhibitors is a critical step for interpreting cell-based data and guiding inhibitor optimization. Herein, a HPLC-MS based protocol was developed to determine inhibitor cellular bioavailability. This generalizable protocol allows determination of the accurate intracellular concentrations and characterization of various properties of inhibitors including the extra- and intracellular stability, the dose- and time-dependence of the intracellular concentrations, the cell permeability, and the nonspecific binding with the cell culture plates, the extracellular matrices, and the cell membrane. The inhibitors of the protein-protein interactions, bromodomains, and the β-catenin/B-cell lymphoma 9 (BCL9) interaction were used to examine the protocol, and the cellular bioavailability of the inhibitors in cancer cells was determined. High nonspecific binding and low cellular uptake were observed for two bromodomain inhibitors. The two β-catenin/BCL9 inhibitors had low nonspecific binding but different cellular uptake. These inhibitors exhibited different stability kinetics in 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.