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Through an extensive SAR optimization
2024-08-06

Through an extensive SAR optimization campaign with the 4-((2-hydroxy-3-methoxybenzyl)amino)-benzenesulfonamide-based scaffold researchers have developed ML355 ((N-benzo[d]thiazol-2-yl)-4((2-hydroxy-3 methoxybenzyl)amino)benzenesulfonamide) [5]. ML355 is a nonreductive, noncompetitive, reversible 12
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Some members from the AAAP
2024-08-06

Some members from the AAAP family, namely the AUX1 and the LAX proteins, transport auxin instead of amino acids [48]. While there is some structural relationship between IAA and Trp, the substrate recognition characteristics seem different for these proteins: the auxins do not have any amino group
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Liaohe River situates in the
2024-08-06

Liaohe River situates in the southwestern part of Northeast China and flows through Liaoning Province. Due to the rapid urbanization and industrialization, Liaohe River has become one of the most polluted rivers in China. Multitudinous organic pollutants that can induce toxicity to organisms such as
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The only psychostimulant treatment option
2024-08-06

The only psychostimulant treatment option in Turkey is methylphenidate (Çetin et al., 2015). It is broken down by carboxylase enzyme (CES1) (Sun et al., 2004). From the point of pharmacokinetics, it may be suggested that CES1 gene polymorphisms may be the key responsible factors in patients resistan
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Based on the observation that antipsychotic drugs increase H
2024-08-06

Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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The first suggestions that the cleaved intracellular domain
2024-08-06

The first suggestions that the cleaved intracellular domain of APP, AICD, might transit to the nucleus and hence selectively regulate gene transcription arose from analogies with the Notch receptor signalling system where similar intra-membrane proteolysis occurs [84], [85] and it was later confirme
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br In our experience br History of ER and ACh
2024-08-06

In our experience History of ER and ACh tests As shown in Table 1, Stein et al. first reported the usefulness of intravenous injection of ER in diagnosing coronary insufficiency in 1949 [16]. In 1972, the first ER spasm provocation test was employed at the Cleveland Clinic during cardiac cathe
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As mentioned above variation of the A
2024-08-05

As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to Moxifloxacin (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having comparable
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If the lack of specificity and the high
2024-08-05

If the lack of specificity and the high pleiotropy may represent a problem in view of the potential chemotherapeutic features of autophagy-inducing agents, it Dimesna may switch into an advantage in the case of chemopreventive strategies. In fact, as non-pharmacologic interventions such as limited
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MLN another selective Aurora A
2024-08-05

MLN8237, another selective Aurora-A inhibitor is said to be more potent than MLN8054 and to cause less benzodiazepine-like side effects based on structure modulation by the addition of a methoxy group to either end of the MLN8054 molecule. It was studied [62] in a once daily (QD) schedule for 7 days
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The inhibition of ACLY induces an anticancer effect that
2024-08-05

The inhibition of ACLY induces an anticancer effect that has been reported to be involved in mitochondrial reactive oxygen species (ROS) generation [14], [16], dual blockade of mitogen-activated protein kinase and phosphatidylinositol-3-kinase/AKT pathways [11], and the glycolytic phenotype of tumor
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Telomerase action at the telomere is highly regulated
2024-08-05

Telomerase action at the telomere is highly regulated; it preferentially elongates the shortest telomeres, and recruitment of the enzyme complex to the telomere occurs in mid-S phase of the cell cycle (Bianchi and Shore, 2007, Britt-Compton et al., 2009, Teixeira et al., 2004, Hemann et al., 2001, T
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Mechanistically it was soon realized that in undead cells
2024-08-05

Mechanistically, it was soon realized that in undead cells, Dronc promotes the activation of Jun-N-terminal kinase (JNK) signaling as the major inducer of AiP [25], [28] (Fig. 2B,C). However, it has been unknown for a long time how active Dronc promotes JNK signaling. Recently, it was reported that
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It has been demonstrated that the
2024-08-05

It has been demonstrated that the hallmarks of pulmonary fibrosis are a loss of endothelial function and subsequent activation of the immune system, which is considered as a direct outcome affected by intracellular pro-inflammatory responses [26]. Thus, inhibition of early inflammation could be an i
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pgc-1α inhibitor Furthermore because most of foods
2024-08-05

Furthermore, because most of foods and beverages have been consumed after processing, researchers have focused on the effects of processing (e.g. blanching, cooking, drying, cooling, freezing, high-pressure treatment, pulsed electric field) on total antioxidant capacity of foods. In general, there w
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