ArticleBioorganic & medicinal chemistry2010
Binding of curcumin and its long chain derivatives to the activator binding domain of novel protein kinase C.
Article in Bioorganic & medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 72 citations in OpenAlex.
- Mechanistic insights into the anti-inflammatory effects of isocoronarin D associated with reduced PKCδ and PI3K/Akt signalling in LPS-activated macrophages.Inflammopharmacology · 2026Article
- Microwave-Assisted, Solid-State Procedure to Covalently Conjugate Hyaluronic Acid to Curcumin: Validation of a Green Synthetic Protocol.ACS polymers Au · 2024Article
- Formulation of the novel structure curcumin derivative-loaded solid lipid nanoparticles: synthesis, optimization, characterization and anti-tumor activity screeningDrug delivery · 2022Article
- Bioactive Effects of Curcumin in Human Immunodeficiency Virus Infection Along with the Most Effective Isolation Techniques and Type of Nanoformulations.International journal of nanomedicine · 2022Review
- Binding of quercetin and curcumin to human serum albumin in aqueous dimethyl sulfoxide and in aqueous ethanol.Journal of thermal analysis and calorimetry · 2022Article
- Amphiphilic Small-Molecule Assemblies to Enhance the Solubility and Stability of Hydrophobic Drugs.ACS omega · 2020Article
- Tunable Release of Curcumin with an In Silico-Supported Approach from Mixtures of Highly Porous PLGA Microparticles.Materials (Basel, Switzerland) · 2020Article
- In vitro anti-inflammatory effects of curcumin on mast cell-mediated allergic responses via inhibiting FcεRI protein expression and protein kinase C delta translocation.Cytotechnology · 2020Article
- Bioactivity of Curcumin on the Cytochrome P450 Enzymes of the Steroidogenic Pathway.International journal of molecular sciences · 2019Article
- Design, synthesis, and evaluation of curcumin analogues as potential inhibitors of bacterial sialidase.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- Gallic Acid Content in Taiwanese Teas at Different Degrees of Fermentation and Its Antioxidant Activity by Inhibiting PKCδ Activation: In Vitro and in Silico Studies.Molecules (Basel, Switzerland) · 2016Article
- Polyphenol compounds and PKC signaling.Biochimica et biophysica acta · 2016Review
- Curcumin, a natural antioxidant, acts as a noncompetitive inhibitor of human RNase L in presence of its cofactor 2-5A in vitro.BioMed research international · 2014Article
- Article
- Multitargeting by curcumin as revealed by molecular interaction studies.Natural product reports · 2011Review
- A curcumin direct protein biosensor for cell-free prototyping.Engineering biologyArticle
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Protein kinase C (PKC) is a family of serine/threonine kinases that play a central role in cellular signal transduction. The second messenger diacylglycerol having two long carbon chains acts as the endogenous ligand for the PKCs. Polyphenol curcumin, the active constituent of Curcuma longa is an anti-cancer agent and modulates PKC activity. To develop curcumin derivatives as effective PKC activators, we synthesized several long chain derivatives of curcumin, characterized their absorption and fluorescence properties and studied their interaction with the activator binding second cysteine-rich C1B subdomain of PKCdelta, PKCepsilon and PKCtheta. Curcumin (1) and its C16 long chain analog (4) quenched the intrinsic fluorescence of PKCdeltaC1B, PKCepsilonC1B and PKCthetaC1B in a manner similar to that of PKC activator 12-O-tetradecanoylphorbol 13-acetate (TPA). The EC(50)s of the curcumin derivatives for fluorescence quenching varied in the range of 4-11 microM, whereas, EC(50)s for TPA varied in the range of 3-6 microM. Fluorescence emission maxima of 1 and 4 were blue shifted and the fluorescence anisotropy values were increased in the presence of the C1B domains in a manner similar to that shown by the fluorescent analog of TPA, sapintoxin-D, confirming that they were bound to the proteins. Molecular docking of 1 and 4 with novel PKC C1B revealed that both the molecules form hydrogen bonds with the protein residues. The present result shows that curcumin and its long chain derivatives bind to the C1B subdomain of novel PKCs and can be further modified structurally to improve its binding and activity.
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Registered trials
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