ArticleBiochimica et biophysica acta2015
Alcohol binding in the C1 (C1A+C1B) domain of protein kinase C epsilon.
Article in Biochimica et biophysica acta, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 17 citations in OpenAlex.
- Alcohol use disorder-associated pain: clinical and preclinical evidence.Alcohol (Fayetteville, N.Y.) · 2025Review
- Zapotin mitigates breast cancer progression by targeting PKCε mediated glycolytic pathway regulation.BMC cancer · 2025Article
- Alcohol Use Disorder: Neurobiology and Therapeutics.Biomedicines · 2022Review
- Effect of ethanol on Munc13-1 C1 in Membrane: A Molecular Dynamics Simulation Study.Alcoholism, clinical and experimental research · 2020Article
- Nicotine and alcohol: the role of midbrain dopaminergic neurons in drug reinforcement.The European journal of neuroscience · 2019Review
- Identification of alcohol-binding site(s) in proteins using diazirine-based photoaffinity labeling and mass spectrometry.Chemical biology & drug design · 2019Article
- Ethanol-Induced Changes in PKCε: From Cell to Behavior.Frontiers in neuroscience · 2018Review
- Review
- Resveratrol inhibits phorbol ester-induced membrane translocation of presynaptic Munc13-1.Biochimica et biophysica acta. General subjects · 2017Article
- Curcumin Inhibits Protein Kinase Cα Activity by Binding to Its C1 Domain.Biochemistry · 2016Article
- Shedding Light on Anesthetic Mechanisms: Application of Photoaffinity Ligands.Anesthesia and analgesia · 2016Review
- Drugs to Treat Alcohol Dependence-A Perspective.Journal of addiction and dependence · 2016Article
- Ethanol-induced enhancement of inhibitory synaptic transmission in the rat spinal substantia gelatinosa.Molecular painArticle
- Article
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2 authors at 1 institution in 1 country.
Funding
Abstract
backgroundAlcohol regulates the expression and function of protein kinase C epsilon (PKCε). In a previous study we identified an alcohol binding site in the C1B, one of the twin C1 subdomains of PKCε (Das et al., Biochem. J., 421, 405-13, 2009).
methodsIn this study, we investigated alcohol binding in the entire C1 domain (combined C1A and C1B) of PKCε. Fluorescent phorbol ester, SAPD and fluorescent diacylglycerol (DAG) analog, dansyl-DAG were used to study the effect of ethanol, butanol, and octanol on the ligand binding using fluorescence resonance energy transfer (FRET). To identify alcohol binding site(s), PKCεC1 was photolabeled with 3-azibutanol and 3-azioctanol, and analyzed by mass spectrometry. The effects of alcohols and the azialcohols on PKCε were studied in NG108-15 cells.
resultsIn the presence of alcohol, SAPD and dansyl-DAG showed different extent of FRET, indicating differential effects of alcohol on the C1A and C1B subdomains. Effects of alcohols and azialcohols on PKCε in NG108-15 cells were comparable. Azialcohols labeled Tyr-176 of C1A and Tyr-250 of C1B. Inspection of the model structure of PKCεC1 reveals that these residues are 40Å apart from each other indicating that these residues form two different alcohol binding sites.
conclusionsThe present results provide evidence for the presence of multiple alcohol-binding sites on PKCε and underscore the importance of targeting this PKC isoform in developing alcohol antagonists.
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