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In order to increase the oral bioavailability abiraterone is
2025-02-07
In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral Foretinib of abiraterone acetate (156), it is recommended that this drug should be taken on an
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Previous studies have demonstrated that
2025-02-07
Previous studies have demonstrated that the expression of the Aurora B gene is maximally increased at G2/M phage during mitosis (Honda et al., 2003, Fu et al., 2007, Goldenson and Crispino, 2015), and exhibits an extraordinary upregulation in a number of human cancers (Fu et al., 2007, Kollareddy et
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histone methyltransferase In PMCA Mg favors the conversion
2025-02-07
In PMCA, Mg2+ favors the conversion E1P → E2P [13] and, as in SERCA [11], it accelerates the phosphorylation displacing the E1–E2 equilibrium towards E1. In SERCA, Sørensen et al. [41], proposed that ATP reacts by an associative mechanism mediated by two Mg2+ ions to form an aspartyl-phosphorylated
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Our previous studies and others have
2025-02-07
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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The functional similarity between GPR and APLNR ie both can
2025-02-07
The functional similarity between GPR25 and APLNR, ie both can be activated by Apelin and Apela and are coupled to Gi-cAMP signaling pathway (Fig. 2, Fig. 3, Fig. 4), strongly suggests that GPR25 signaling may play important physiological and pathological roles in vertebrates more or less similar to
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br Materials and methods br Results and
2025-02-07
Materials and methods Results and discussion Conclusion The preparation of acrylic nanoparticles as aminosugar carriers could not be achieved by direct functionalization of poly(t-butyl acrylate) particles with saccharide groups. A four-step procedure starting from a protected derivative of
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Introduction Heterotrimeric G proteins mediate
2025-02-07
Introduction Heterotrimeric Gαβγ proteins mediate signal transduction through seven-transmembrane domain receptors. In response to neurotransmitters or hormones, activated receptors bind GTP via the Gα subunit leading to the dissociation of Gα from the Gβγ dimer. G proteins regulate the levels of s
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AMPK is an essential player
2025-02-06
AMPK is an essential player in adiponectin signaling pathway that regulates energy metabolism. The fact that suppression of AMPK activity by compound C largely diminished candesartan-mediated inhibition of NFκB via blocking AT1 also suggests that the AT1-mediated effect is at least partly resulted f
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In the isolated right atrium activation of muscarinic recept
2025-02-06
In the isolated right atrium, activation of muscarinic receptors and adenosine receptors may block the generation of action potentials in the sinoatrial node, inducing cardiac arrest (Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5) (Camara et al., 2015, Campbell et al., 1989). Physiologically, this conditio
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br Patients and methods The severity
2025-02-06
Patients and methods The severity of disease documented at each outpatient visit was graded according to the modified Osserman classification: grade I, focal disease (e.g. restricted to ocular muscles); grade II, generalised disease that is mild (IIa) or moderate (IIb); grade III, severe generali
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The major strength of this study is the large
2025-02-06
The major strength of this study is the large sample size which increases the statistical power to detect the likely subtle differences in peripheral methylation observed in psychiatric disorders (Olsson et al., 2010). Larger studies help provide more robust estimates of true associations, as small
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Song et al reported series of triazolylsalicylamide derivati
2025-02-06
Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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For the TSH receptor signaling
2025-02-06
For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as Acyclovir depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Continued sign
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br Experimental Procedures Additional information can be fou
2025-02-06
Experimental Procedures Additional information can be found in Supplemental Experimental Procedures. Author Contributions Acknowledgments We thank all members of Lab of Health Chemistry for helpful discussions. This work was supported by Grant-in-Aid for Scientific Research (KAKENHI) from
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Here the so called alkali assay
2025-02-06
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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