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In the mammalian brain synapse formation
2023-12-12

In the mammalian brain, synapse formation is followed by a period of synapse refinement, and autophagy has been shown to play an important role in this process. For example, Tang and colleagues found that autophagy is required for the developmental pruning of dendritic spines, and that this pruning
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gap27 Roles of Aurora kinases in directly activating multipl
2023-12-12

Roles of Aurora kinases in directly activating multiple oncogenic pathways and promoting proliferation as well as transformation have also been demonstrated. Aurora-A has been shown to up-regulate telomerase reverse transcriptase mRNA through c-myc [26]. The kinase was also implicated in activating
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PF also a dual Aurora A
2023-12-12

PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly SKI II for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD was defined
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Matthew et al synthesized and carried out
2023-12-12

Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that Cdk2/Cyclin Inhibitory Peptide I australia 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phos
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Co is an essential element for life
2023-12-12

Co is an essential element for life in minute amounts [5]. The human adult contains about 1.1mg Co with the daily requirement of 0.1μg/day. Co is a component of vitamin B12. Co induces erythropoietin and blocks iodine uptake by the thyroid, controls the transfer of enzymes like homocysteine methyltr
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Among all the polysaccharide derivatives cationic carbohydra
2023-12-12

Among all the polysaccharide derivatives, cationic carbohydrate polymers such as quaternary ammonium salts and quaternary phosphonium salts have been the most popular and most efficient target 4EGI-1 in medical applications [24] and water treatment [25]. Recently, quaternary phosphonium salts were r
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Incubation of the aortic segments of
2023-12-12

Incubation of the aortic segments of rats with indomethacin significantly decreased the vasoconstrictor response to Phe but only in HgCl2-treated group (Fig. 9A,B), as indicated by dAUC values (Fig. 9E). Co-treatment with losartan once again proved to be effective and prevented the increased partici
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To date attention has been
2023-12-12

To date, attention has been directed towards new molecular targets in luminal phenotype (ER-positive), such as CDK4/6 and, to a lesser extent, androgen receptor (AR) pathways [8]. While the role of CDK4/6 has been elucidated and their inhibitors have shown a benefit in luminal BC, the role of AR in
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Testosterone can be converted into estrogens by
2023-12-12

Testosterone can be converted into estrogens by aromatase action. Aromatase is encoded by CYP19, belongs to cytochrome P450 superfamily, and synthesizes estradiol (E2) and estrone (E1) from testosterone and androstenedione respectively (Fig. 1). Aromatase is expressed in the ORS of anagen hair folli
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Camptothecin AMPK is a central regulator of
2023-12-12

AMPK is a central regulator of cell growth, migration, metabolism, autophagy, and cell polarity [20], [21], [22], [23]. It is highly conserved in eukaryotes and functions as the primary sensor of intracellular adenosine nucleotides [24]. When intracellular ATP levels decrease, AMPK is activated to g
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Neural activity resulting from sensory
2023-12-12

Neural activity resulting from sensory experience is required for the refinement and maturation of neural circuits during cortical critical periods. This refinement is thought to be important for functional optimization of primary sensory cortices, enabling critical functions such as feature detecti
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The ORR obtained with crizotinib on our cohort
2023-12-12

The ORR obtained with crizotinib on our cohort was low compared to other studies, such as the prospective studies of A. Shaw et al. (ORR = 65% in second line), B. Solomon et al. (ORR = 74% in first line) and the more comparable large retrospective study of M. Duruisseaux et al. on the French CLINAL
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Gratifyingly compound also demonstrated improved
2023-12-12

Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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Capsaicin br Role of OCT in
2023-12-12

Role of OCT3 in histamine clearance Histamine is a powerful neuromodulator, as well as a regulator of immune processes and vascular tone in the central nervous system (Gross, 1981; Haas et al., 2008; Jutel et al., 2006). In contrast to 5-HT and the catecholamines, a high-affinity transporter for
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br Methods br Results br Discussion Chronic stress renders
2023-12-12

Methods Results Discussion Chronic stress renders individuals vulnerable to diseases, and this effect might be, at least partially, mediated by stress hormone-induced immunosuppression. Therefore, investigating the effects of catecholamines on immune CP-809101 hydrochloride is of high relev
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