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In recent years the higher lipophilicity
2023-08-10
In recent years, the ‘higher lipophilicity’-thus-‘better performance’ tenet, derived from the polar paradox theory applied to micro-structured media, was challenged by novel and unexpected experimental results. In particular, the synthesis of many complete series of fatty Mifepristone esters of nat
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Here we found that AMPK
2023-08-10
Here we found that AMPK directly phosphorylates EZH2 at Thr311 to disrupt its interaction with SUZ12 and to inhibit PRC2 enzymatic activity, which is supported by the increased expression of PRC2-repressed genes. Furthermore, the T311E-EZH2 mutant that mimics AMPK-mediated phosphorylation status su
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br Results and discussion br
2023-08-10
Results and discussion Conclusion The tyrosine kinase ALK represents one of the most successful molecular targets for the development of precise medicine to treat stratified subgroups of cancer patients. Three generations of ALK inhibitors have been awarded the FDA's approval or are being exte
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br Discussion Mycobacterium tuberculosis infection is a main
2023-08-10
Discussion Mycobacterium tuberculosis infection is a main threat to mankind, with one third of the world population being infected. [9] Over nine million new cases of tuberculosis and two million deaths from this disease occur yearly worldwide. [10] The rising incidence of tuberculosis over the l
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Polyphenols like flavonoids have the potential to
2023-07-03
Polyphenols like flavonoids have the potential to penetrate into lipid bilayers which is vital for enabling protection against oxidation. Rosmarinic Dioscin is a natural polyphenol antioxidant isolated from Sphaeranthus amaranthoides. Polyphenols can inhibit the propagation of lipid oxidation by tw
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These PrPIF are detected in untreated
2023-06-27
These PrPIF are detected in untreated dacomitinib extracts but are consistently enriched following proteinase K (PK) treatment. The biochemical characterization of pathologic PrP has been carried out in most hereditary PrP cerebral amyloidosis associated with PrP mutations and the biochemical PrP pa
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Recently different kinds of A aggregation inhibitors have
2023-06-26
Recently, different kinds of Aβ aggregation inhibitors have been reported, including small molecules [8], peptides [9], and nanoparticles (NPs) [10]. The working mechanisms of the inhibitors are mostly to bind or adsorb Aβ molecules and to affect the conformational changes followed by blocking the a
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Adiponectin also works on AdipoR
2023-06-19
Adiponectin also works on AdipoR1, inducing extracellular Ca2+ influx necessary for activation of Ca2+/calmodulin-dependent protein kinase kinase (CaMKK)β, AMPK (Fig. 1). This step is then followed by activation of SirT1 and increased expression and decreased acetylation of PPARγ coactivator (PGC)-1
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Adiponectin also works on AdipoR
2023-06-19
Adiponectin also works on AdipoR1, inducing extracellular Ca2+ influx necessary for activation of Ca2+/calmodulin-dependent protein kinase kinase (CaMKK)β, AMPK (Fig. 1). This step is then followed by activation of SirT1 and increased expression and decreased acetylation of PPARγ coactivator (PGC)-1
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Topiroxostat mg In the present study the alternative splicin
2023-06-15
In the present study, the alternative splicing of several nAChR subunits was identified in the oriental migratory locust (Locusta migratoria manilensis Meyen), a serious worldwide pest to agricultural production and also a model insect species [5]. Several α subunits were tried to co-express with ra
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Five alternatively spliced isoforms of ATX have been
2023-06-13
Five alternatively-spliced isoforms of ATX have been described and all are catalytically active [16], [17]. The original ATX described in 1992 is termed ATXα, whereas the most abundant isoform is ATXβ and is the same isoform responsible for plasma lysoPLD activity [18]. Full length ATX is synthesize
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The surprising finding of our study
2023-06-13
The surprising finding of our study is that human M1 macrophages stimulated by LPS express ALOX15B to high levels. So far 12/15-lipoxygenase activity was only reported for IL-4 stimulated anti-phlogistic M2 macrophages [9] but not for the classically activated M1 macrophages. Our data suggest that s
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br Experimental procedures Adk tg Adktm tg UbiAdk mice were
2023-06-01
Experimental procedures Adk-tg (Adktm1−/−:tg(UbiAdk) mice were created by breeding a loxP-flanked Adk transgene under the control of a human ubiquitin promoter into ADK knockout mice (Fedele et al., 2005,). Fb-Adk-def (Adktm1−/−:tg(UbiAdk):Emx1-Cre-tg3) mice were generated by pairing Emx1-Cre-tg3
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Toxicity is the main reason for the failure at all
2023-05-30
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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A similar circuit between pyramidal neurons and
2023-05-30
A similar circuit between pyramidal neurons and SST interneurons is also prevalent in layers 2/3 of the cortex. The synapses onto SST interneurons, however, are functionally weak, raising questions about their computational power. In the first set of experiments, Urban-Ciecko et al. (2018) show that
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