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Screening a selection of analogues from this library
2024-08-08
Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to gw web 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demonstrated >50% i
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br Results and discussion br Conclusion
2024-08-08
Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen gpr40 agonist o
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This project was funded by the
2024-08-08
This project was funded by the University of the Philippines Diliman through the Natural Sciences Research Institute with grant No. CHE-09-2-02. Introduction There is compelling evidence for an anti-inflammatory effect of 12- and 15-lipoxygenases through the generation of lipid mediators involve
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br Aromatase the key enzyme for
2024-08-08
Aromatase: the key enzyme for estrogen formation in adipose tissue Estrogens are synthesized from androgens by aromatase, a member of the cytochrome P450 superfamily, which is the rate-limiting enzyme in estrogen biosynthesis (Santen et al, 2009, Simpson et al, 1994). At the cellular level, aroma
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On the other hand our study permits to draw
2024-08-08
On the other hand, our study permits to draw general conclusions about the complex functional pattern of C4HT, C8HT and C12HT, in comparison with the parent molecule HT and two reference compounds like Trolox and vitamin E. Table 1 summarizes the results obtained in the present investigation (for th
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br Future view and implications The selection
2024-08-08
Future view and implications The selection and spread of multi(drug)-resistant microorganisms over the last decades has become a major and global public health concern [35]. Two growing threats originating from the fungal kingdom, i.e. Aspergillus fumigatus and Candida auris[36], [37], re-emphasi
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br Results br Discussion Using primarily an
2024-08-07
Results Discussion Using primarily an electrophysiological analysis of dysbindin-deficient hippocampal neurons in cultures and slices, we have uncovered a previously unreported role for dysbindin in enhancing CA3–CA1 AMPAR-mediated transmission. An earlier study, however, has reported a reduct
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br Materials and methods br Results br
2024-08-07
Materials and methods Results Discussion Intracellular metabolic pathways of sugar, such as glycolysis and TCA cycle, provide material and energy for the synthesis of other substances, including amino acids. Thus, the content of sugars and their metabolic pathways are important for amino ek
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br Acknowledgments and Disclosures br
2024-08-07
Acknowledgments and Disclosures Introduction In mammals, ejaculated sperm requires a finite period of residence in the female reproductive tract to become competent for fertilization (Visconti et al., 1995a, Visconti et al., 1995b). Once oocytes are matured, it is important for these cells to
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Compound mg was purified as an amorphous colourless powder
2024-08-07
Compound 3 (29 mg) was purified as an amorphous, colourless powder. Molecular formula C20H28O4 was established by HRESIMS (Fig. S11) and corroborated with 1H and 13C NMR spectroscopic data (Table 1). IR spectrum showed bands for hydroxyl (3433 cm−1) and carbonyl (1686 cm−1) groups. 13C NMR spectrum
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br Acknowledgments The authors would like
2024-08-07
Acknowledgments The authors would like to thank Ms. Ashley Davis for her administrative assistance in preparing this article and Mr. Dan Beck for his artistic contributions to Fig. 1. Introduction Acetylcholine is the most abundant neurotransmitter in the central nervous system (CNS) of insec
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CK is considered a central controller of cellular energy hom
2024-08-07
CK is considered a central controller of cellular energy homeostasis that catalyzes the reversible transfer of a phosphoryl group from ATP to adenosine diphosphate (ADP) and creatine to produce PCr [5]. This enzyme builds up a large pool of rapidly diffusing PCr for temporal and spatial buffering of
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Tumor suppressor ARF regulates the activity of p by inhibiti
2024-08-07
Tumor suppressor ARF regulates the activity of p53 by inhibiting the functions of Mdm2. ARF is induced by hyperproliferative signals emanating from oncogenic Ras, overexpressed c-myc, and from deregulated E2F . ARF prevents p53 degradation and leads to increased p53 function by sequestering Mdm2 to
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The transcription factor activator protein AP is a redox sen
2024-08-06
The transcription factor activator protein-1 (AP-1) is a redox-sensitive transcription factor whose activity is controlled by agents that perturb intracellular thiol concentrations [10,11]. AP-1 is mainly composed of Jun, Fos, and ATF protein dimers [12,13]. AP-1 mediates the regulation of numerous
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The incremental reduction albeit not
2024-08-06
The incremental reduction, albeit not statistically significant, in collagen I with LCZ696 compared to perindopril treated animals, may therefore be related to a more compliant ventricle in LCZ696-treated animals. This is not so surprising given the incremental anti-fibrotic effect of the active met
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