Investigation of inhibition of human glucose 6-phosphate dehydrogenase by some 99mTc chelators by<i>in silico</i>and<i>in vitro</i>methods

Şahin, Ali; Şentürk, Murat; Salmas, Ramin Ekhteiari; Durdağı, Serdar; Ayan, Arif Kürşad; Karagölge, Ali; Mestanoğlu, Mert

doi:10.1080/14756366.2016.1178735

Cited by 9 publications

(2 citation statements)

References 35 publications

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“…Considering that G6PD usually only operates around 2% of its maximum potential in non-transformed cells [ 58 ] while in cancer cells this percentage is significantly higher, it is vital to highlight the key role of G6PD in the proliferation of tumor cells. Indeed, several other studies in various tissues also demonstrated the importance of G6PD in cell viability [ 10 , 45 , 59 ].…”

Section: Discussionmentioning

confidence: 93%

Glutamine Modulates Expression and Function of Glucose 6-Phosphate Dehydrogenase via NRF2 in Colon Cancer Cells

et al. 2021

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Nucleotide pools need to be constantly replenished in cancer cells to support cell proliferation. The synthesis of nucleotides requires glutamine and 5-phosphoribosyl-1-pyrophosphate produced from ribose-5-phosphate via the oxidative branch of the pentose phosphate pathway (ox-PPP). Both PPP and glutamine also play a key role in maintaining the redox status of cancer cells. Enhanced glutamine metabolism and increased glucose 6-phosphate dehydrogenase (G6PD) expression have been related to a malignant phenotype in tumors. However, the association between G6PD overexpression and glutamine consumption in cancer cell proliferation is still incompletely understood. In this study, we demonstrated that both inhibition of G6PD and glutamine deprivation decrease the proliferation of colon cancer cells and induce cell cycle arrest and apoptosis. Moreover, we unveiled that glutamine deprivation induce an increase of G6PD expression that is mediated through the activation of the nuclear factor (erythroid-derived 2)-like 2 (NRF2). This crosstalk between G6PD and glutamine points out the potential of combined therapies targeting oxidative PPP enzymes and glutamine catabolism to combat colon cancer.

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Section: Discussionmentioning

confidence: 93%

Glutamine Modulates Expression and Function of Glucose 6-Phosphate Dehydrogenase via NRF2 in Colon Cancer Cells

et al. 2021

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“…Interaction between the compound and Phe171 may lead to inhibition of the enzyme by interfering with the interaction between the residue and the substrate. Several G6PDs have demonstrated similar modes of interaction [58,59]. On the other hand, the binding modes showed that compound 52 with the 4-nitrobenzylidene group may inhibit the enzyme by closely interacting with Glu151 residue.…”

Section: Targetsmentioning

confidence: 99%

Anticancer Profile of Rhodanines: Structure–Activity Relationship (SAR) and Molecular Targets—A Review

2022

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The rhodanine core is a well-known privileged heterocycle in medicinal chemistry. The rhodanines, as subtypes of thiazolidin-4-ones, show a broad spectrum of biological activity, including anticancer properties. This review aims to analyze the anticancer features of the rhodanines described over the last decade in the scientific literature. The structure–activity relationship of rhodanine derivatives, as well as some of the molecular targets, were discussed. The information contained in this review could be of benefit to the design of new, effective small molecules with anticancer potential among rhodanine derivatives or their related heterocycles.

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Citrus Honeys from Three Different Regions of Turkey: HPLC‐DAD Profiling and in Vitro Enzyme Inhibition, Antioxidant, Anti‐Inflammatory and Antimicrobial Properties with Chemometric Study

Tel‐Çayan,

Çiftçi,

Taş‐Küçükaydın

et al. 2023

Chemistry & Biodiversity

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The objectives of the present study are to compare the phenolic profiles and biological activities of 15 citrus honey samples from three different locations in Turkey using a chemometric approach. The HPLC‐DAD analysis was used to determine phenolic profiles. Nineteen phenolic compounds were identified. Gallic acid (107.14‐717.04 μg/g) was recorded as the predominant compound. AF (Antalya‐Finike) had the highest antioxidant activity in ABTS•+ (IC50: 18.01±0.69 mg/mL), metal chelating (IC50: 6.20±0.19 mg/mL) and CUPRAC (A0.50: 12.05±0.68 mg/mL) assays, while it revealed the best anti‐inflammatory activity against COX‐2 (17.28±0.22%) and COX‐1 (43.28±0.91%). AM (Antalya‐Manavgat) was the most active in β‐carotene‐linoleic acid (IC50: 10.05±0.19 mg/mL), anti‐urease (38.90±0.69%), anti‐quorum sensing and antimicrobial activities. AKO1 (Adana‐Kozan‐1) in DPPH• (IC50: 34.25±0.81 mg/mL) assay, AKU1 (Antalya‐Kumluca‐1) in tyrosinase inhibition activity (37.73±0.38%) assay, AKU2 (Antalya‐Kumluca‐2) in AChE (10.55±0.63%) and BChE (9.18±0.45%) inhibition activity assays showed the best activity. Chemometric tools were applied to the phenolic compositions and biological properties. PCA and HCA ensured that 15 citrus honey samples were grouped into 3 clusters. The results showed that myricetin, kaempferol, vanillin, protocatechuic acid, rosmarinic acid, rutin, vanillic acid, gallic acid, catechin and p‐hydroxyphenyl acetic acid are phenolic compounds that can be used in the classification of citrus honeys.

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Investigation of inhibition of human glucose 6-phosphate dehydrogenase by some 99mTc chelators byin silicoandin vitromethods

Cited by 9 publications

References 35 publications

Glutamine Modulates Expression and Function of Glucose 6-Phosphate Dehydrogenase via NRF2 in Colon Cancer Cells

Glutamine Modulates Expression and Function of Glucose 6-Phosphate Dehydrogenase via NRF2 in Colon Cancer Cells

Anticancer Profile of Rhodanines: Structure–Activity Relationship (SAR) and Molecular Targets—A Review

Citrus Honeys from Three Different Regions of Turkey: HPLC‐DAD Profiling and in Vitro Enzyme Inhibition, Antioxidant, Anti‐Inflammatory and Antimicrobial Properties with Chemometric Study

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