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Many ruthenium complexes were tested as potential anticancer
2024-11-20

Many ruthenium complexes were tested as potential anticancer agents and two complexes, namely NAMI-A (trans-[imH] [RuCl4(dmso-S)(im)]; im, imidazole) and KP1019 (trans-[indH][RuCl4(ind)2]; ind, indazole) have successfully entered clinical trials [27], [28]. NAMI-A is selectively active against metas
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A high throughput screening campaign led to the
2024-11-20

A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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It is now well established that the cumulative exposure to
2024-11-20

It is now well established that the cumulative exposure to endogenous estrogens throughout a woman's life, mainly due to her reproductive history, has an impact on the risk of hormone-dependent breast cancer (Lambertini et al., 2016). Prolonged exposure to estrogens in the case of early age at menar
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Here the so called alkali assay
2024-11-20

Here the so-called alkali assay [18] is proposed as a method to be applied directly on the purified recombinant enzyme sharing the same structural and functional features of the wild-type enzyme [19], [20], [21] using its physiological substrate androstenedione. The assay that was already successful
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br Materials and methods br Results A first
2024-11-20

Materials and methods Results A first series of experiments explored whether the Ampkα1 isoform is involved in the regulation of cardiac Pkcζ. To this end, HL-1 cardiomyocytes were transfected with a construct encoding constitutively active Prkaa1T183D (CAα1) or with the empty vector as contro
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In this study Rb increased the phosphorylation
2024-11-20

In this study, Rb1 increased the phosphorylation of p38 MAPK and Akt and macrophage phagocytosis of bacteria in mouse lung cells, consistent with the in vitro results. A recent study showed that Rb1 diminished the severity of lung injury in rats exposed to LPS. Rb1 inhibited the LPS-induced increase
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br Does TIPARP contribute to the
2024-11-20

Does TIPARP contribute to the diverse species sensitivity to TCDD toxicity? In chick embryo hepatocytes TIPARP was reported to mediate the TCDD-dependent suppression of hepatic gluconeogenesis, by reducing cellular NAD+ levels and reducing PCK1 expression, suggesting that ADP-ribosylation enhance
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In brief serotonin can interact with classes of
2024-11-19

In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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In summary the role of HT and differe http
2024-11-19

In summary, the role of 5-HT and different types of 5-HTRs in gating plasticity induction in neocortical circuits remains unclear, with variable and seemingly contradictory effects reported for LTP induction in cortical sensory fields (e.g., V1, enhanced LTP: Inaba et al., 2009, Kojic et al., 1997,
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trans-AUCB The results also showed that
2024-11-19

The results also showed that the A3 receptor agonist increased the phosphorylated levels of Akt, leading to activation of the PI3K/Akt pathway. A3 trans-AUCB stimulation has protective effects against RGC death following ischemia-reperfusion, glutamate toxicity, and optic nerve transection models (
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Steroidal CYP inhibitors can further be classified based
2024-11-19

Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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glucocorticoid receptor antagonist As summarized in Fig auto
2024-11-19

As summarized in Fig. 1, autophagy up-regulation in terms of Beclin 1 induction, increase of LC3 II and p62 down-regulation were observed between 24 and 72 h of cell incubation, this coinciding with the end of the period 27-OH caused slight reduction of cell viability and proliferation as previously
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ATP citrate lyase ACLY is a cytosolic
2024-11-19

ATP citrate lyase (ACLY) is a cytosolic enzyme that catalyzes the generation of acetyl-CoA from citrate [15]. Acetyl-CoA is the building block for the biosynthesis of fatty acids and cholesterol, and also serves as a substrate of the acetylation reaction of various molecules, including histones and
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Inflammations lead to the perturbation of aromatase enzyme w
2024-11-19

Inflammations lead to the perturbation of aromatase enzyme [112], which normally is responsible for a broad array of critical functions. Chemotherapy targets this enzyme, so this treatment option is never side-effect-free and not fully-effective. Therefore, the mankind should be careful so as not to
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Our previous studies and others
2024-11-19

Our previous studies and others have identified that the inhalational anesthetic isoflurane induces neuronal apoptosis via [Ca2+]i overload through the opening of synaptic voltage-dependent calcium channels (VDCCs) and the excessive Ca2+ release from the endoplasmic reticulum (Zhao et al., 2011; Zha
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