Curcumin is the active ingredient found in turmeric, a common spice used all over the world. The beneficial effects of curcumin intake have been investigated extensively, but a new paper published in Proceedings from the National Academy of Sciences reports a new target for curcumin.
Researchers report evidence of the protein kinase dual-specificity tyrosine regulated kinase 2 (DYRK2) as a receptor for curcumin. In vitro biochemical assays show that curcumin had an IC50 value of 5 nM against DYRK2. Additionally in an assay against 144 different protein kinases, curcumin is a selective ligand for DYRK2, with an IC50 10 fold greater than the next nearest kinase. The authors further confirm DYRK2 as the target of curcumin by overexpressing DYRK2 in HEK293T cells, and noting a decrease in phosphorylation of tyrosine 25 in the RPT3 subunit of the 26S proteasome, the major target of DYRK2. Additionally, the researchers publish a crystal structure of DYRK2 with curcumin bound in the active site, noting the important amino acid residues for binding.
In cell-based experiments, curcumin shows anti-cancer capabilities. Curcumin shows anti-proliferative, anti-invasive and apoptotic tendencies in MDA-MB-231 triple negative breast cancer cells and HaCaT cells. The researchers also found a synergistic relationship between curcumin and carfilzomib, a proteasome inhibitor marketed for the treatment of triple negative breast cancer patients and multiple myeloma. Curcumin in conjunction with other proteasome inhibitors could make an interesting combination for the treatment of disease.
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Banerjee S, Chenggong J, Mayefield JE, Goel A et al. “Ancient drug curcumin impedes 26S proteasome activity by direct inhibition of dual-specificity tyrosine-regulated kinase 2.” Proc. Nat. Acad. Sci. 2018, 115(32): 8155-8160. doi: 10.1073/pnas.1806797115.