Effects of novel quercetin derivatives on sarco/endoplasmic reticulum Ca2+-ATPase

Blaskovic, D; Držík, Filip; Viskupičová, Jana; Veverka, Miroslav; Horáková, Ľubica

doi:10.1016/j.freeradbiomed.2012.08.193

Cited by 3 publications

(4 citation statements)

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“…In this case nitration may be associated with decreases in SERCA activity. Disruption of these oxidative modifications has been proposed as a potential therapeutic strategy to alter SERCA activity in disease models [347]. This could have potential use to either induce activity for promotion of apoptosis in cancer cells, or inhibit SERCA mediated apoptosis in cases of cardiovascular disease.…”

Section: Redox Regulation Of Er and Mitochondrial Ca2+ Modulatorsmentioning

confidence: 99%

Crosstalk between calcium and reactive oxygen species signaling in cancer

2017

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The interplay between Ca2+ and reactive oxygen species (ROS) signaling pathways is well established, with reciprocal regulation occurring at a number of subcellular locations. Many Ca2+ channels at the cell surface and intracellular organelles, including the endoplasmic reticulum and mitochondria are regulated by redox modifications. In turn, Ca2+ signaling can influence the cellular generation of ROS, from sources such as NADPH oxidases and mitochondria. This relationship has been explored in great depth during the process of apoptosis, where surges of Ca2+ and ROS are important mediators of cell death. More recently, coordinated and localized Ca2+ and ROS transients appear to play a major role in a vast variety of pro-survival signaling pathways that may be crucial for both physiological and pathophysiological functions. While much work is required to firmly establish this Ca2+-ROS relationship in cancer, existing evidence from other disease models suggests this crosstalk is likely of significant importance in tumorigenesis. In this review, we describe the regulation of Ca2+ channels and transporters by oxidants and discuss the potential consequences of the ROS-Ca2+ interplay in tumor cells.

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Section: Redox Regulation Of Er and Mitochondrial Ca2+ Modulatorsmentioning

confidence: 99%

Crosstalk between calcium and reactive oxygen species signaling in cancer

2017

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“…The remaining derivatives did not exhibit any effect at concentrations up to 50 μM; above that, weak inhibitory or moderate stimulatory effect on SERCA activity was observed . Nevertheless, the derivative compound 43 showed marked improvement in SERCA-inhibiting activity …”

Section: Non-terpenoid Serca Inhibitorsmentioning

confidence: 92%

“…Furthermore, at least two flavonoid-binding sites that may take part in the cooperative inhibition of SERCA were predicted for compound 40; one of them is in the nucleotide-binding domain and the other is at the interface of the nucleotidebinding domain and the actuator domain. 199 Further research into compound 40 derivatives was done by Blasǩovičet al 200,201 Contrary to the findings of Ogunbayo et al, 70 the IC 50 value of compound 40 was equal to 150 μM while diquercetin (43, Figure 18) almost abolished the SERCA activity at the same concentration. Out of another eight tested quercetin derivatives, only 1,4,5-tri(chloropivatoyl)quercetin (44, Figure 18) possessed significant inhibition properties.…”

Section: Non-terpenoid Serca Inhibitorsmentioning

confidence: 94%

“…201 Nevertheless, the derivative compound 43 showed marked improvement in SERCA-inhibiting activity. 200 Another flavonoid examined for SERCA inhibitory activity was rutin and its fatty acid derivatives 40 (45, Figure 19). Rutin can protect SERCA from the inhibitory effect resulting from treatment of SERCA with hypochloric acid or peroxynitrite.…”

Section: Non-terpenoid Serca Inhibitorsmentioning

confidence: 99%

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Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective

et al. 2020

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The sarco/endoplasmic reticulum calcium ATPase (SERCA), which plays a key role in the maintenance of Ca 2+ ion homeostasis, is an extensively studied enzyme, the inhibition of which has a considerable impact on cell life and death decision. To date, several SERCA inhibitors have been thoroughly studied and the most notable one, a derivative of the sesquiterpene lactone thapsigargin, is gradually approaching a clinical application. Meanwhile, new compounds with SERCA-inhibiting properties of natural, synthetic, or semisynthetic origin are being discovered and/or developed; some of these might also be suitable for the development of new drugs with improved performance. This review brings an up-to-date comprehensive overview of recently discovered compounds with the potential of SERCA inhibition, discusses their mechanism of action, and highlights their potential clinical applications, such as cancer treatment.

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