ArticleJournal of medicinal chemistry2014
Thienoquinolines as novel disruptors of the PKCε/RACK2 protein-protein interaction.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 34 citations in OpenAlex.
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- Protein kinase C epsilon contributes to chronic mechanoreflex sensitization in rats with heart failure.The Journal of physiology · 2025Article
- Synthesis of Tricyclic and Tetracyclic Lactone Derivatives of Thieno[2,3-Molecules (Basel, Switzerland) · 2025Article
- PKCε inhibition prevents ischemia‑induced dendritic spine impairment in cultured primary neurons.Experimental and therapeutic medicine · 2023Article
- Mo-Catalyzed One-Pot Synthesis of N-Polyheterocycles from Nitroarenes and Glycols with Recycling of the Waste Reduction Byproduct. Substituent-Tuned Photophysical Properties.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- Drug Repositioning Inferred from E2F1-Coregulator Interactions Studies for the Prevention and Treatment of Metastatic Cancers.Theranostics · 2019Article
- Oxidative stress associated with aging activates protein kinase Cε, leading to cilia slowing.American journal of physiology. Lung cellular and molecular physiology · 2018Article
- Hierarchical virtual screening approaches in small molecule drug discovery.Methods (San Diego, Calif.) · 2015Review
Corrections and comments
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Authors and funding
12 authors at 6 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ten protein kinase C (PKC) isozymes play divergent roles in signal transduction. Because of sequence similarities, it is particularly difficult to generate isozyme-selective small molecule inhibitors. In order to identify such a selective binder, we derived a pharmacophore model from the peptide EAVSLKPT, a fragment of PKCε that inhibits the interaction of PKCε and receptor for activated C-kinase 2 (RACK2). A database of 330 000 molecules was screened in silico, leading to the discovery of a series of thienoquinolines that disrupt the interaction of PKCε with RACK2 in vitro. The most active molecule, N-(3-acetylphenyl)-9-amino-2,3-dihydro-1,4-dioxino[2,3-g]thieno[2,3-b]quinoline-8-carboxamide (8), inhibited this interaction with a measured IC50 of 5.9 μM and the phosphorylation of downstream target Elk-1 in HeLa cells with an IC50 of 11.2 μM. Compound 8 interfered with MARCKS phosphorylation and TPA-induced translocation of PKCε (but not that of PKCδ) from the cytosol to the membrane. The compound reduced the migration of HeLa cells into a gap, reduced invasion through a reconstituted basement membrane matrix, and inhibited angiogenesis in a chicken egg assay.
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