2018
DOI: 10.1113/ep086826
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Abstract: The protein kinase casein kinase 2 (CK2) is a ubiquitously expressed serine or threonine kinase known to phosphorylate a number of substrates. The aim of this study was to assess the effect of CK2 inhibition on spontaneous and oxytocin-induced uterine contractions in 19 day pregnant mice. The CK2 inhibitor CX-4945 elicited a concentration-dependent relaxation in late pregnant mouse uterus. CX-4945 and another selective CK2 inhibitor, apigenin, also inhibited the oxytocin-induced contractile response in late pr… Show more

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Cited by 7 publications
(9 citation statements)
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“…In this work, we have shown that the apigenin upregulation of functional CD26/DPPIV at the cell surface of intestinal epithelial cells (a) is consistent across multiple well‐differentiated human cell lines, (b) is due to cellular redistribution rather than a change in expression, (c) may be reproduced by multiple inhibitors of CK2 kinase activity, (d) does not involve downregulation of CK2 protein, and (e) is abrogated by siRNA knockdown of available CK2. It is well established that apigenin can inhibit CK2 activity, and indeed, it is used experimentally as a CK2 inhibitor (Ahmad, Wang, & Ahmed, 2006; Jung, Kim, & Lee, 2014; Kim et al., 2018; Kroonen et al., 2012; Suhas et al., 2018). We conclude that the ability of apigenin to upregulate CD26/DPPIV involves inhibition of the kinase activity of CK2 and is dependent upon the presence of functional CK2 enzyme.…”
Section: Resultsmentioning
confidence: 99%
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“…In this work, we have shown that the apigenin upregulation of functional CD26/DPPIV at the cell surface of intestinal epithelial cells (a) is consistent across multiple well‐differentiated human cell lines, (b) is due to cellular redistribution rather than a change in expression, (c) may be reproduced by multiple inhibitors of CK2 kinase activity, (d) does not involve downregulation of CK2 protein, and (e) is abrogated by siRNA knockdown of available CK2. It is well established that apigenin can inhibit CK2 activity, and indeed, it is used experimentally as a CK2 inhibitor (Ahmad, Wang, & Ahmed, 2006; Jung, Kim, & Lee, 2014; Kim et al., 2018; Kroonen et al., 2012; Suhas et al., 2018). We conclude that the ability of apigenin to upregulate CD26/DPPIV involves inhibition of the kinase activity of CK2 and is dependent upon the presence of functional CK2 enzyme.…”
Section: Resultsmentioning
confidence: 99%
“…However, it is not certain that apigenin influences cellular behaviors, including regulation of interactions with the extracellular matrix, cellular contractility, and the levels of molecules including CD26/DPPIV (Kim et al., 2018; Lefort & Blay, 2011; Suhas et al., 2018), solely through inhibition of CK2. The effects of apigenin in cellular experimental systems are distinct from synthetic CK2 inhibitors such as CX‐4945 (Suhas et al., 2018). Furthermore, the CK2 interactions of flavonoid inhibitors such as quercetin and fisetin differ from those of synthetic inhibitors such as emodin and TBB in terms of the residues impacted (Sarno et al., 2002).…”
Section: Resultsmentioning
confidence: 99%
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“…L-type calcium channels are implicated in the excitation-contraction coupling in cardiac, skeletal and smooth muscle, in the regulation of Ca 2+ homeostasis and secretion, tissue development, neuron excitability, excitation-transcription coupling and in learning and memory in the brain, reviewed in ( 104 ). Furthermore, L-type Ca 2+ channel activation results in uterine contraction of mice, the activation of which is suppressed by inhibition of CK2( 58 ). Ca v 1.1 is the L-type Ca 2+ channel present in the skeletal muscle and Ca v 1.2 is the L-type channel present in the heart.…”
Section: Ck2 and Calcium Channelsmentioning
confidence: 99%
“…CK2 is ubiquitously scattered within eukaryotic cells (53)(54)(55)(56) and is present on the cell surface as an ecto-kinase (57). Moreover, CK2 is located in lipid rafts of brain synaptosomes and uterine cell membranes (58,59). In brain synaptosomes, inhibition of CK2 resulted in an enhanced neurotransmitter release (59).…”
Section: Introductionmentioning
confidence: 99%