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As aforementioned this study aimed
2024-08-19
As aforementioned, this study aimed to design, synthesize and investigate aromatase inhibitory and anti-breast cancer activities of N,N′-disubstituted thiourea derivatives. Based on the attractive phenotypic molecule 1, the synthetic N,N′-disubstituted thioureas have been designed including monothio
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br Conclusions br Funding This work was supported by a
2024-08-19
Conclusions Funding This work was supported by a Finnish government subsidy for health science research [grant numbers TYH2012141, TYH 2013218, and TYH 2014216]; the SSAC Foundation [grant numbers SLS-504141 and SLS-693781]; and the Paulo Foundation. The funding sources had no involvement in s
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Detailed analysis of the dose
2024-08-19
Detailed analysis of the dose dependence of Aβ effects revealed that at low amounts, Aβ can also act as a positive regulator of presynaptic activity, enhancing the neurotransmitter release probability and increasing the neuronal excitability [2]. The facilitator effects of low Aβ dose on excitatory
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Initially DPP DPP and prolyl
2024-08-19
Initially, DPP4, DPP7, and prolyl tripeptidyl peptidase A (PtpA) were the only exopeptidases identified in P. gingivalis. These share substrates according to their altered specificities, as DPP4 is highly specific for Pro at the penultimate position from the N-terminus (P1 position), though it accep
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We further analyzed selected hit compounds
2024-08-17
We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma BMS777607 were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotubercidin was employed as
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As noted earlier the PfkB family of
2024-08-17
As noted earlier, the PfkB family of carbohydrate kinases can phosphorylate the hydroxymethyl group of a wide variety of sugar moieties [1], [3]. Recent searches of the Swiss-Prot database with the two conserved sequence motifs found in these proteins (Accession nos. PS00583 and PS00584) identified
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Acknowledgements The work was supported by grants from Swedi
2024-08-17
Acknowledgements The work was supported by grants from Swedish Research Council (J.Z.H.) (A.R.M.). We thank Protein Science Facility (PSF), Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden. We thank Prof. Ralf Morgenstern (Department for Environmental Medic
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br Author contributions br Conflict of interest br
2024-08-17
Author contributions Conflict of interest Acknowledgements This work was supported by the National Natural Science Foundation of China (81502276), Major Projects of Science and Technology of Health and Family Planning Commission of Hunan Province (A2017013), the Natural Science Foundation o
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Having established the structural requirements
2024-08-17
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vit
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Another factor that is involved in
2024-08-17
Another factor that is involved in the severity of EAE is apoptosis signal-regulating kinase 1 (ASK1), which is one of a growing number of mitogen-activated protein kinase (MAPK) kinase kinases identified in the upstream of the c-Jun N-terminal kinase and p38 MAPK pathways [12]. We previously repor
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br Abbreviations br Acknowledgements This work
2024-08-17
Abbreviations Acknowledgements This work was supported by grants from the National Institutes of Health (R01GM114168) and the Office of Naval Research (N000141210773) awarded to J.C·H and National Cancer Institute (5P30CA16059) Cancer Center Support Grant in support of Massey Cancer Center Pro
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ARG I is one of the most important mammalian enzymes
2024-08-17
ARG I is one of the most important mammalian enzymes responsible for nitrogen metabolism since it comprises the main route for the elimination of excess nitrogen resulting from amino Silicristin and nucleotide metabolism [18]. ARG I deficiency leads to hyperargininemia, characterized by progressive
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br Materials and methods br Results A first
2024-08-17
Materials and methods Results A first series of experiments explored whether the Ampkα1 isoform is involved in the regulation of cardiac Pkcζ. To this end, HL-1 cardiomyocytes were transfected with a construct encoding constitutively active Prkaa1T183D (CAα1) or with the empty vector as contro
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On the other hand oxygen concentration in tumor tissue also
2024-08-16
On the other hand, oxygen concentration in tumor tissue also depends on its consumption rate by tumor cells, which decrease will also lead to alleviation of hypoxia. This fact is not taken into account in the majority of studies on the topic, although it is well-known that antiangiogenic therapy doe
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Optical coherence tomography angiography is another promisin
2024-08-16
Optical coherence tomography angiography is another promising method for the assessment of corneal neovascularization. This relatively new modality is not yet widely used in part because of current limitations in the definition of images produced, lack of functional information, and inability to det
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